-
2
-
-
0000669419
-
Comprehensive survey of combinatorial library synthesis: 2001
-
Dolle R.E. Comprehensive survey of combinatorial library synthesis: 2001. J. Comb. Chem. 4:2002;369-418.
-
(2002)
J. Comb. Chem.
, vol.4
, pp. 369-418
-
-
Dolle, R.E.1
-
3
-
-
0036007206
-
Recent developments in combinatorial organic synthesis
-
Ganesan A. Recent developments in combinatorial organic synthesis. Drug Discov. Today. 7:2002;47-55.
-
(2002)
Drug Discov. Today
, vol.7
, pp. 47-55
-
-
Ganesan, A.1
-
5
-
-
0036652153
-
Solid phase compound library synthesis in drug design and development
-
Edwards P.J., Morrell A.I. Solid phase compound library synthesis in drug design and development. Curr. Opin. Drug Discov. Develop. 5:2002;594-605.
-
(2002)
Curr. Opin. Drug Discov. Develop
, vol.5
, pp. 594-605
-
-
Edwards, P.J.1
Morrell, A.I.2
-
6
-
-
0037859908
-
Fast purification essential to drug discovery
-
April
-
Potts W: Fast purification essential to drug discovery. Drug Discov Devel 2000, April:59.
-
(2000)
Drug Discov Devel
, pp. 59
-
-
Potts, W.1
-
7
-
-
0036603591
-
Combinatorial synthesis of natural products
-
Nielsen J. Combinatorial synthesis of natural products. Curr. Opin. Chem. Biol. 6:2002;297-305.
-
(2002)
Curr. Opin. Chem. Biol.
, vol.6
, pp. 297-305
-
-
Nielsen, J.1
-
8
-
-
0037119336
-
From protein domains to drug candidates-natural products as guiding principles in the design and synthesis of compound libraries
-
Breinbauer R., Vetter I.R., Waldmann H. From protein domains to drug candidates-natural products as guiding principles in the design and synthesis of compound libraries. Angew. Chem. Int. Ed. Engl. 41:2002;2878-2890.
-
(2002)
Angew. Chem. Int. Ed. Engl.
, vol.41
, pp. 2878-2890
-
-
Breinbauer, R.1
Vetter, I.R.2
Waldmann, H.3
-
9
-
-
0037522387
-
Better genomics through chemistry
-
March
-
Sender AJ: Better genomics through chemistry. Genome Technol 2002, March:40-50.
-
(2002)
Genome Technol
, pp. 40-50
-
-
Sender, A.J.1
-
10
-
-
0037859943
-
Collaborations Spur Merck's targeted discovery
-
March
-
Karet G: Collaborations Spur Merck's targeted discovery. Drug Discov Devel 2000, March:28-32.
-
(2000)
Drug Discov Devel
, pp. 28-32
-
-
Karet, G.1
-
11
-
-
0002446997
-
Combinatorial chemistry: Novel strategies for drugs and materials
-
Borman S. Combinatorial chemistry: novel strategies for drugs and materials. Chem. Eng. News. 8:2001;49-58.
-
(2001)
Chem. Eng. News
, vol.8
, pp. 49-58
-
-
Borman, S.1
-
12
-
-
0037124196
-
Drugs, leads, and drug-likeness: An analysis of some recently launched drugs
-
Proudfoot J.R. Drugs, leads, and drug-likeness: an analysis of some recently launched drugs. Bioorg. Med. Chem. Lett. 12:2002;1647-1650.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1647-1650
-
-
Proudfoot, J.R.1
-
13
-
-
0034677966
-
Drug discovery: A historical perspective
-
Drews J. Drug discovery: a historical perspective. Science. 287:2000;1960-1964.
-
(2000)
Science
, vol.287
, pp. 1960-1964
-
-
Drews, J.1
-
14
-
-
0035914606
-
Discovery and synthesis of a new class of cathepsin K inhibitors
-
Smith R.A., Bhargava A., Browe C., Chen J., Dumas J., Hatoum-Mokdad H., Romero R. Discovery and synthesis of a new class of cathepsin K inhibitors. Bioorg. Med. Chem. Lett. 11:2001;2951-2954.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2951-2954
-
-
Smith, R.A.1
Bhargava, A.2
Browe, C.3
Chen, J.4
Dumas, J.5
Hatoum-Mokdad, H.6
Romero, R.7
-
15
-
-
0035811452
-
4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: The effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters
-
Hagen S.E., Domagala J., Gajda C., Lovdahl M., Tait B.D., Wise E., Holler T., Hupe D., Nouhan C., Urumov A.et al. 4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters. J. Med. Chem. 44:2001;2319-2332.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2319-2332
-
-
Hagen, S.E.1
Domagala, J.2
Gajda, C.3
Lovdahl, M.4
Tait, B.D.5
Wise, E.6
Holler, T.7
Hupe, D.8
Nouhan, C.9
Urumov, A.10
-
16
-
-
0035943435
-
Selective cleavage of D-Ala-D-Lac by small molecules: Re-sensitizing resistant bacteria to Vancomycin
-
New approach in the fight against vancomycin-resistant bacteria discovered through the screening of tripeptide combinatorial libraries
-
Chiosis G., Boneca I.G. Selective cleavage of D-Ala-D-Lac by small molecules: Re-sensitizing resistant bacteria to Vancomycin. Science. 293:2001;1484-1487 New approach in the fight against vancomycin-resistant bacteria discovered through the screening of tripeptide combinatorial libraries.
-
(2001)
Science
, vol.293
, pp. 1484-1487
-
-
Chiosis, G.1
Boneca, I.G.2
-
17
-
-
17944376779
-
1,4-Disubstitued imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI)
-
Heerding D.A., Chan G., DeWolf W.E., Fosberry A.P., Janson C.A., Jaworski D.D., McManus E., Miller W.H., Moore T.D., Payne D.J.et al. 1,4-Disubstitued imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI). Bioorg. Med. Chem. Lett. 11:2001;2061-2065.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2061-2065
-
-
Heerding, D.A.1
Chan, G.2
DeWolf, W.E.3
Fosberry, A.P.4
Janson, C.A.5
Jaworski, D.D.6
McManus, E.7
Miller, W.H.8
Moore, T.D.9
Payne, D.J.10
-
18
-
-
0037013429
-
ATP channel openers (KCOs)
-
ATP channel openers (KCOs). Bioorg. Med. Chem. Lett. 12:2002;1481-1484.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1481-1484
-
-
Drizin, I.1
Holladay, M.W.2
Yi, L.3
Zhang, H.Q.4
Gopalakrishnan, S.5
Gopalakrishnan, M.6
Whiteaker, K.L.7
Buckner, S.A.8
Sullivan, J.P.9
Carroll, W.A.10
-
19
-
-
0035829434
-
Discovery of a series of nonpeptide small molecules that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins
-
The authors discuss their experience in tracking down active constituents in HTS hits, which were stored in DMSO, a frequent and tedious process experienced by many groups
-
Chen C., Zhu Y.-F., Liu X.-J., Lu Z.-X., Xie Q., Ling N. Discovery of a series of nonpeptide small molecules that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins. J. Med. Chem. 44:2001;4001-4010 The authors discuss their experience in tracking down active constituents in HTS hits, which were stored in DMSO, a frequent and tedious process experienced by many groups.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 4001-4010
-
-
Chen, C.1
Zhu, Y.-F.2
Liu, X.-J.3
Lu, Z.-X.4
Xie, Q.5
Ling, N.6
-
20
-
-
0035818922
-
New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models
-
Szczepankiewicz B.G., Liu G., Jae H.S., Tasker A.S., Gunawardana I.W., von Geldern T.W., Gwaltney S.L., Wu-Wong J.R., Gehrke L., Chiou W.J.et al. New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models. J. Med. Chem. 44:2001;4416-4430.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 4416-4430
-
-
Szczepankiewicz, B.G.1
Liu, G.2
Jae, H.S.3
Tasker, A.S.4
Gunawardana, I.W.5
Von Geldern, T.W.6
Gwaltney, S.L.7
Wu-Wong, J.R.8
Gehrke, L.9
Chiou, W.J.10
-
21
-
-
0035821394
-
Identification of subtype selective humanPPARα agonist through parallel-array synthesis
-
Brown P.J., Stuart L.W., Hurley K.P., Lewis M.C., Winegar D.A., Wilson J.G., Wilkison W.O., Ittoop O.R., Willson T.M. Identification of subtype selective humanPPARα agonist through parallel-array synthesis. Bioorg. Med. Chem. Lett. 11:2001;1225-1227.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1225-1227
-
-
Brown, P.J.1
Stuart, L.W.2
Hurley, K.P.3
Lewis, M.C.4
Winegar, D.A.5
Wilson, J.G.6
Wilkison, W.O.7
Ittoop, O.R.8
Willson, T.M.9
-
22
-
-
0035942162
-
A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport
-
An excellent example of the use of large, combinatorial split-mix libraries in facilitating the drug-discovery process
-
Oliver W.R., Shenk J.L., Snaith M.R., Russell C.S., Plunket K.D., Bodkin N.L., Lewis M.C., Winegar D.A., Sznaidman M.L., Lambert M.H. A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport. Proc. Natl Acad. Sci. USA. 98:2001;5306-5311 An excellent example of the use of large, combinatorial split-mix libraries in facilitating the drug-discovery process.
-
(2001)
Proc. Natl Acad. Sci. USA
, vol.98
, pp. 5306-5311
-
-
Oliver, W.R.1
Shenk, J.L.2
Snaith, M.R.3
Russell, C.S.4
Plunket, K.D.5
Bodkin, N.L.6
Lewis, M.C.7
Winegar, D.A.8
Sznaidman, M.L.9
Lambert, M.H.10
-
23
-
-
18244374489
-
The discovery of acylated β-amino acids as potent and orally bioavailable VLA-4 antagonists
-
Lin L.S.et al. The discovery of acylated β-amino acids as potent and orally bioavailable VLA-4 antagonists. Bioorg. Med. Chem. Lett. 12:2002;611-614.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 611-614
-
-
Lin, L.S.1
-
24
-
-
0035935194
-
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists
-
Hagmann W.K., Durette P.L., Lanza T., Kevin N.J., de Laszlo S.E., Kopka I.E., Young D., Magriotis P.A., Li B., Lin L.S.et al. The discovery of sulfonylated dipeptides as potent VLA-4 antagonists. Bioorg. Med. Chem. Lett. 11:2001;2709-2713.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2709-2713
-
-
Hagmann, W.K.1
Durette, P.L.2
Lanza, T.3
Kevin, N.J.4
De Laszlo, S.E.5
Kopka, I.E.6
Young, D.7
Magriotis, P.A.8
Li, B.9
Lin, L.S.10
-
25
-
-
0037124203
-
Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists
-
Chen L., Trilles R., Miklowski D., Huang T.-N., Fry D., Campbell R., Rowan K., Schwinge V., Tilley J.W. Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists. Bioorg. Med. Chem. Lett. 12:2002;1679-1682.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1679-1682
-
-
Chen, L.1
Trilles, R.2
Miklowski, D.3
Huang, T.-N.4
Fry, D.5
Campbell, R.6
Rowan, K.7
Schwinge, V.8
Tilley, J.W.9
-
26
-
-
0035935206
-
Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists
-
Barrow J.C., Nantermet P.G., Selnick H.G., Glass K.L., Ngo P.L., Young M.B., Pellicore J.M., Breslin M.J., Hutchinson J.H., Freidinger R.M.et al. Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists. Bioorg. Med. Chem. Lett. 11:2001;2691-2696.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2691-2696
-
-
Barrow, J.C.1
Nantermet, P.G.2
Selnick, H.G.3
Glass, K.L.4
Ngo, P.L.5
Young, M.B.6
Pellicore, J.M.7
Breslin, M.J.8
Hutchinson, J.H.9
Freidinger, R.M.10
-
27
-
-
18244372993
-
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1)
-
Nantermet P.G., Barrow J.C., Lundell G.F., Pellicore J.M., Rittle K.E., Young M., Freidinger R.M., Connolly T.M., Condra C., Karczewski J.et al. Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1). Bioorg. Med. Chem. Lett. 12:2002;319-323.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 319-323
-
-
Nantermet, P.G.1
Barrow, J.C.2
Lundell, G.F.3
Pellicore, J.M.4
Rittle, K.E.5
Young, M.6
Freidinger, R.M.7
Connolly, T.M.8
Condra, C.9
Karczewski, J.10
-
28
-
-
0035921058
-
Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole based peptide mimetics by anchoring to a secondary amide
-
Zhang H.-C., McComsey D.F., White K.B., Addo M.F., Andrade-Gordan P., Derian C.K., Oksenberg D., Maryanoff B.E. Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole based peptide mimetics by anchoring to a secondary amide. Bioorg. Med. Chem. Lett. 11:2001;2105-2109.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2105-2109
-
-
Zhang, H.-C.1
McComsey, D.F.2
White, K.B.3
Addo, M.F.4
Andrade-Gordan, P.5
Derian, C.K.6
Oksenberg, D.7
Maryanoff, B.E.8
-
29
-
-
0035899192
-
The first potent and selective inhibitors of the glycine transporter type 2
-
Caulfield W.L., Collie I.T., Dickins R.S., Epemolu O., McGuire R., Hill D.R., McVey G., Morphy J.R., Rankovic Z., Sundaram H. The first potent and selective inhibitors of the glycine transporter type 2. J. Med. Chem. 44:2001;2679-2682.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2679-2682
-
-
Caulfield, W.L.1
Collie, I.T.2
Dickins, R.S.3
Epemolu, O.4
McGuire, R.5
Hill, D.R.6
McVey, G.7
Morphy, J.R.8
Rankovic, Z.9
Sundaram, H.10
-
30
-
-
18344379671
-
Use of parallel-synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors
-
Choi C., Li J.H., Vaal M., Thomas C., Limburg D., Wu Y.Q., Chen Y., Soni R., Scott C., Ross D.T.et al. Use of parallel-synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors. Bioorg. Med. Chem. Lett. 12:2002;1421-1428.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1421-1428
-
-
Choi, C.1
Li, J.H.2
Vaal, M.3
Thomas, C.4
Limburg, D.5
Wu, Y.Q.6
Chen, Y.7
Soni, R.8
Scott, C.9
Ross, D.T.10
-
31
-
-
18344393965
-
Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides
-
Wei L., Wu Y., Wilkinson D.E., Chen Y., Soni R., Scott C., Ross D.T., Guo H., Howorth P., Valentine H.et al. Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides. Bioorg. Med. Chem. Lett. 12:2002;1429-1433.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1429-1433
-
-
Wei, L.1
Wu, Y.2
Wilkinson, D.E.3
Chen, Y.4
Soni, R.5
Scott, C.6
Ross, D.T.7
Guo, H.8
Howorth, P.9
Valentine, H.10
-
32
-
-
18244364639
-
A combinatorial library of Indinavir analogues and its in vitro and in vivo studies
-
The authors demonstrate the utility of testing split-mix sample sets in a dog model for PK profiling
-
Cheng Y., Rano T.A., Huening T.T., Zhang F., Lu Z., Schleif W.A., Gabryelski L., Olsen D.B., Stahlhut M., Kuo L.C.et al. A combinatorial library of Indinavir analogues and its in vitro and in vivo studies. Bioorg. Med. Chem. Lett. 12:2002;529-532 The authors demonstrate the utility of testing split-mix sample sets in a dog model for PK profiling.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 529-532
-
-
Cheng, Y.1
Rano, T.A.2
Huening, T.T.3
Zhang, F.4
Lu, Z.5
Schleif, W.A.6
Gabryelski, L.7
Olsen, D.B.8
Stahlhut, M.9
Kuo, L.C.10
-
33
-
-
18644384334
-
2′
-
An excellent example of the use of combinatorial libraries to help solve unfavorable PK properties
-
2′ Bioorg. Med. Chem. Lett. 12:2002;2855-2858 An excellent example of the use of combinatorial libraries to help solve unfavorable PK properties.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2855-2858
-
-
Raghavan, S.1
Yang, Z.2
Mosley, R.T.3
Schleif, W.A.4
Gabryelski, L.5
Olsen, D.B.6
Stahlhut, M.7
Kuo, L.C.8
Emini, E.A.9
Chapman, K.T.10
Tata, J.R.11
-
34
-
-
18344386398
-
Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1)
-
Norman B.H., Gruber J.M., Hollinshead S.P., Wilson J.W., Starling J.J., Law K.L., Self T.D., Tabas L.B., Williams D.C., Paul D.C.et al. Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1). Bioorg. Med. Chem. Lett. 12:2002;883-886.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 883-886
-
-
Norman, B.H.1
Gruber, J.M.2
Hollinshead, S.P.3
Wilson, J.W.4
Starling, J.J.5
Law, K.L.6
Self, T.D.7
Tabas, L.B.8
Williams, D.C.9
Paul, D.C.10
-
35
-
-
0035848396
-
3 prostanoid receptor by use of solid-support chemistry
-
3 prostanoid receptor by use of solid-support chemistry. Bioorg. Med. Chem. Lett. 11:2001;747-749.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 747-749
-
-
Juteau, H.1
Gareau, Y.2
Labelle, M.3
Lamontagne, S.4
Tremblay, N.5
Carriere, M.-C.6
Sawyer, N.7
Denis, D.8
Metters, K.M.9
-
36
-
-
18644374700
-
3 prostanoid receptor
-
3 prostanoid receptor. Bioorg. Med. Chem. Lett. 12:2002;2583-2586.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2583-2586
-
-
Gallant, M.1
Carriere, M.C.2
Chateauneuf, A.3
Denis, D.4
Gareau, Y.5
Godbout, C.6
Greig, G.7
Juteau, H.8
Lachance, N.9
Lacombe, P.10
-
37
-
-
0035899191
-
Development of serine protease inhibitors displaying a multicentered short (<2.3 Å) hydrogen bond binding mode: Inhibitors of urokinase-type plasminogen activator and factor Xa
-
The discovery of a new class of non-covalent serine protease inhibitors demonstrating a unique mode of binding. Also, nicely illustrates the idea of a platform technology approach to drug discovery
-
Verner E., Katz B.A., Spencer J.R., Allen D., Hataye J., Hruzewicz W., Hui H.C., Kolesnikov A., Li Y., Luong C.et al. Development of serine protease inhibitors displaying a multicentered short (<2.3 Å) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa. J. Med. Chem. 44:2001;2753-2771 The discovery of a new class of non-covalent serine protease inhibitors demonstrating a unique mode of binding. Also, nicely illustrates the idea of a platform technology approach to drug discovery.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2753-2771
-
-
Verner, E.1
Katz, B.A.2
Spencer, J.R.3
Allen, D.4
Hataye, J.5
Hruzewicz, W.6
Hui, H.C.7
Kolesnikov, A.8
Li, Y.9
Luong, C.10
-
38
-
-
0037025461
-
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinse-type plasminogen activator inhibitors
-
Spencer J.R., McGee D., Allen D., Katz B.A., Luong C., Sendzik M., Squires N., Mackman R.L. 4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinse-type plasminogen activator inhibitors. Bioorg. Med. Chem. Lett. 12:2002;2023-2026.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2023-2026
-
-
Spencer, J.R.1
McGee, D.2
Allen, D.3
Katz, B.A.4
Luong, C.5
Sendzik, M.6
Squires, N.7
Mackman, R.L.8
-
39
-
-
0037030602
-
1-[2-(5-Cyanopyridin-2-yl)amino]-ethylamino]acetyl-2-(S)-pyrrolidine- carbonitrile: A potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties
-
Villhauer E.B., Brinkman J.A., Naderi G.B., Dunning B.E., Mangold B.L., Mone M.D., Russell M.E., Weldon S.C., Hughes T.E. 1-[2-(5-Cyanopyridin-2-yl)amino]-ethylamino]acetyl-2-(S)-pyrrolidine- carbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. J. Med. Chem. 45:2002;2362-2365.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2362-2365
-
-
Villhauer, E.B.1
Brinkman, J.A.2
Naderi, G.B.3
Dunning, B.E.4
Mangold, B.L.5
Mone, M.D.6
Russell, M.E.7
Weldon, S.C.8
Hughes, T.E.9
-
40
-
-
0037194629
-
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151)
-
A good example of the use of libraries to rapidly identify back-up compounds for the HNE inhibitor GW311616A
-
Macdonald S.J., Dowle M.D., Harrison L.A., Clarke G.D., Inglis G.G., Johnson M.R., Shah P., Smith R.A., Amour A., Fleetwood G.et al. Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151). J. Med. Chem. 45:2002;3878-3890 A good example of the use of libraries to rapidly identify back-up compounds for the HNE inhibitor GW311616A.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 3878-3890
-
-
Macdonald, S.J.1
Dowle, M.D.2
Harrison, L.A.3
Clarke, G.D.4
Inglis, G.G.5
Johnson, M.R.6
Shah, P.7
Smith, R.A.8
Amour, A.9
Fleetwood, G.10
-
41
-
-
0037087516
-
Click chemistry in situ: Acetylcholinesterase as a reaction vessel for the selective assembly of a femtomolar inhibitor from an array of building blocks
-
An elegant and insightful approach, which identifies extremely potent AchE inhibitors by allowing the enzyme to catalyze inhibitor formation
-
Lewis W.G., Green L.G., Grynszpan F., Radic Z., Carlier P.R., Taylor P., Finn M.G., Sharpless K.B. Click chemistry in situ: acetylcholinesterase as a reaction vessel for the selective assembly of a femtomolar inhibitor from an array of building blocks. Angew. Chem. Int. Ed. Engl. 41:2002;1053-1056 An elegant and insightful approach, which identifies extremely potent AchE inhibitors by allowing the enzyme to catalyze inhibitor formation.
-
(2002)
Angew. Chem. Int. Ed. Engl.
, vol.41
, pp. 1053-1056
-
-
Lewis, W.G.1
Green, L.G.2
Grynszpan, F.3
Radic, Z.4
Carlier, P.R.5
Taylor, P.6
Finn, M.G.7
Sharpless, K.B.8
-
42
-
-
0037133575
-
Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts
-
One of several papers from these laboratories outlining a successful peptidomimetic approach to inhibiting protein-protein interactions
-
Berg T., Cohen S.B., Desharnais J., Sonderegger C., Maslyar D.J., Goldberg J., Boger D.L., Vogt P.K. Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts. Proc. Natl. Acad Sci. USA. 99:2002;3830-3835 One of several papers from these laboratories outlining a successful peptidomimetic approach to inhibiting protein-protein interactions.
-
(2002)
Proc. Natl. Acad Sci. USA
, vol.99
, pp. 3830-3835
-
-
Berg, T.1
Cohen, S.B.2
Desharnais, J.3
Sonderegger, C.4
Maslyar, D.J.5
Goldberg, J.6
Boger, D.L.7
Vogt, P.K.8
-
43
-
-
0037196281
-
Erythropoietin mimetics derived from solution phase combinatorial libraries
-
Goldberg J., Jin Q., Ambroise Y., Satoh S., Desharnais J., Capps K., Boger D.L. Erythropoietin mimetics derived from solution phase combinatorial libraries. J. Am. Chem. Soc. 124:2002;544-555.
-
(2002)
J. Am. Chem. Soc.
, vol.124
, pp. 544-555
-
-
Goldberg, J.1
Jin, Q.2
Ambroise, Y.3
Satoh, S.4
Desharnais, J.5
Capps, K.6
Boger, D.L.7
-
44
-
-
0037187386
-
Design, synthesis and evaluation of opioid analogues with non-peptidic β-turn scaffold: Enkephalin and endomorphin mimetics
-
Eguchi M., Shen R.Y.W., Shea J.P., Lee M.S., Kahn M. Design, synthesis and evaluation of opioid analogues with non-peptidic β-turn scaffold: enkephalin and endomorphin mimetics. J. Med. Chem. 25:2002;1395-1398.
-
(2002)
J. Med. Chem.
, vol.25
, pp. 1395-1398
-
-
Eguchi, M.1
Shen, R.Y.W.2
Shea, J.P.3
Lee, M.S.4
Kahn, M.5
-
45
-
-
0035821348
-
The identification and characterization of hydrazinyl urea-based antibacterial agents through combinatorial chemistry
-
Wilson L.J., Morris T.W., Wu Q., Renick P.J., Parker C.N., Davis M.C., McKeever H.D., Hershberger P.M., Switzer A.G., Shrum G.et al. The identification and characterization of hydrazinyl urea-based antibacterial agents through combinatorial chemistry. Bioorg. Med. Chem. Lett. 11:2001;1149-1152.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1149-1152
-
-
Wilson, L.J.1
Morris, T.W.2
Wu, Q.3
Renick, P.J.4
Parker, C.N.5
Davis, M.C.6
McKeever, H.D.7
Hershberger, P.M.8
Switzer, A.G.9
Shrum, G.10
-
46
-
-
0037142343
-
Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain
-
Du X.D., Guo C., Hansell E., Doyle P.S., Caffrey C.R., Holler T.P., McKerrow J.H., Cohen F.E. Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain. J. Med. Chem. 45:2002;2695-2707.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2695-2707
-
-
Du, X.D.1
Guo, C.2
Hansell, E.3
Doyle, P.S.4
Caffrey, C.R.5
Holler, T.P.6
McKerrow, J.H.7
Cohen, F.E.8
-
47
-
-
0037046549
-
Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens
-
Jarvest R.L., Berge J.M., Berry V., Boyd H.F., Brown M.J., Elder J.S., Forrest A.K., Fosberry A.P., Gentry D.R., Hibbs M.J.et al. Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens. J. Med. Chem. 45:2002;1960-1962.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 1960-1962
-
-
Jarvest, R.L.1
Berge, J.M.2
Berry, V.3
Boyd, H.F.4
Brown, M.J.5
Elder, J.S.6
Forrest, A.K.7
Fosberry, A.P.8
Gentry, D.R.9
Hibbs, M.J.10
-
48
-
-
17944363800
-
Optimization of a screening lead for Factor VIIa/TF
-
•]
-
•].
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2253-2256
-
-
Young, W.B.1
Kolesnikov, A.2
Rai, R.3
Sprengeler, P.A.4
Leahy, E.M.5
Shrader, W.D.6
Sangalang, J.7
Burgess-Henry, J.8
Spencer, J.9
Elrod, K.10
Cregar, L.11
-
49
-
-
18244388008
-
7 integrin antagonists
-
7 integrin antagonists. Bioorg. Med. Chem. Lett. 12:2002;159-163.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 159-163
-
-
Chang, L.L.1
Truong, Q.2
Mumford, R.A.3
Egger, L.A.4
Kidambi, U.5
Lyons, K.6
McCauley, E.7
Van-Riper, G.8
Vincent, S.9
Schmidt, J.A.10
-
50
-
-
0037119827
-
4-Aminoquinolines as a novel class of NR1/2B subtype selective NMDA receptor antagonists
-
Pinard E., Alanine A., Bourson A., Buttelmann B., Heitz M.-P., Mutel V., Gill R., Trube G., Wyler R. 4-Aminoquinolines as a novel class of NR1/2B subtype selective NMDA receptor antagonists. Bioorg. Med. Chem. Lett. 12:2002;2615-2619.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2615-2619
-
-
Pinard, E.1
Alanine, A.2
Bourson, A.3
Buttelmann, B.4
Heitz, M.-P.5
Mutel, V.6
Gill, R.7
Trube, G.8
Wyler, R.9
-
51
-
-
0035848572
-
Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores
-
Wang G.T., Chen Y., Wang S., Gentles R., Sowin T., Kati W., Muchmore S., Giranda V., Stewart K., Sham H.et al. Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores. J. Med. Chem. 44:2001;1192-1201.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 1192-1201
-
-
Wang, G.T.1
Chen, Y.2
Wang, S.3
Gentles, R.4
Sowin, T.5
Kati, W.6
Muchmore, S.7
Giranda, V.8
Stewart, K.9
Sham, H.10
-
52
-
-
0035938427
-
The discovery of RFI-641 as a potent and selective inhibitor of the respiratory syncytial virus
-
Nikitenko A.A., Raifeld Y.E., Wang T.Z. The discovery of RFI-641 as a potent and selective inhibitor of the respiratory syncytial virus. Bioorg. Med. Chem. Lett. 11:2001;1041-1044.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1041-1044
-
-
Nikitenko, A.A.1
Raifeld, Y.E.2
Wang, T.Z.3
-
53
-
-
0036527429
-
Protein kinases - the major drug targets of the twenty-first century?
-
Cohen P. Protein kinases - the major drug targets of the twenty-first century? Nat. Rev. Drug Discov. 1:2002;309-315.
-
(2002)
Nat. Rev. Drug Discov.
, vol.1
, pp. 309-315
-
-
Cohen, P.1
-
54
-
-
0033813234
-
Discovery of a new class of p38 kinase inhibitors
-
Dumas J., Sibley R., Riedl B., Monahan M.K., Lee W., Lowinger T.B., Redman A.M., Johnson J.S., Kingery-Wood J., Scott W.J.et al. Discovery of a new class of p38 kinase inhibitors. Bioorg. Med. Chem. Lett. 10:2000;2047-2050.
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 2047-2050
-
-
Dumas, J.1
Sibley, R.2
Riedl, B.3
Monahan, M.K.4
Lee, W.5
Lowinger, T.B.6
Redman, A.M.7
Johnson, J.S.8
Kingery-Wood, J.9
Scott, W.J.10
-
55
-
-
18344395134
-
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site
-
Pargellis C., Tong L., Churchill L., Cirillo P.F., Gilmore T., Graham A.G., Grob P.M., Hickey E.R., Moss N., Pav S., Regan J. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat. Struct. Biol. 9:2002;268-272.
-
(2002)
Nat. Struct. Biol.
, vol.9
, pp. 268-272
-
-
Pargellis, C.1
Tong, L.2
Churchill, L.3
Cirillo, P.F.4
Gilmore, T.5
Graham, A.G.6
Grob, P.M.7
Hickey, E.R.8
Moss, N.9
Pav, S.10
Regan, J.11
-
56
-
-
0037019275
-
Pyrazole urea-based inhibitors of p-38 MAP kinase: From lead compound to clinical candidate
-
Discovery of a novel, allosteric binding site for p-38 kinase. An excellent example of a diversity-driven drug-discovery process. Clinical candidate indentified. See also [55]
-
Regan J., Breitfelder S., Cirillo P., Gilmore T., Graham A.G., Hickey E., Klaus B., Madwed J., Moriak M., Moss N.et al. Pyrazole urea-based inhibitors of p-38 MAP kinase: from lead compound to clinical candidate. J. Med. Chem. 45:2002;2994-3008 Discovery of a novel, allosteric binding site for p-38 kinase. An excellent example of a diversity-driven drug-discovery process. Clinical candidate indentified. See also [55].
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2994-3008
-
-
Regan, J.1
Breitfelder, S.2
Cirillo, P.3
Gilmore, T.4
Graham, A.G.5
Hickey, E.6
Klaus, B.7
Madwed, J.8
Moriak, M.9
Moss, N.10
-
57
-
-
0035825364
-
P38 Kinase inhibitors for the treatment of arthritis and osteoporosis: Thienyl, furyl, and pyrrolyl ureas
-
Redman A.M., Johnson J.S., Dally R., Swartz S., Wild H., Paulsen H., Caringal Y., Gunn D., Renick J., Osterhout M.et al. p38 Kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas. Bioorg. Med. Chem. Lett. 11:2001;9-12.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 9-12
-
-
Redman, A.M.1
Johnson, J.S.2
Dally, R.3
Swartz, S.4
Wild, H.5
Paulsen, H.6
Caringal, Y.7
Gunn, D.8
Renick, J.9
Osterhout, M.10
-
58
-
-
0037124174
-
Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor
-
Dumas J., Hatoum-Mokdad H., Sibley R.N., Smith R.A., Scott W.J., Khire U., Lee W., Wood J., Wolanin D., Cooley J.et al. Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor. Bioorg. Med. Chem. Lett. 12:2002;1559-1562.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1559-1562
-
-
Dumas, J.1
Hatoum-Mokdad, H.2
Sibley, R.N.3
Smith, R.A.4
Scott, W.J.5
Khire, U.6
Lee, W.7
Wood, J.8
Wolanin, D.9
Cooley, J.10
-
59
-
-
0035935203
-
Discovery of heterocyclic ureas as a new class of Raf kinase inhibitors: Identification of a second generation lead by a combinatorial chemistry approach
-
Smith R.A., Barbosa J., Blum C.L., Bobko M.A., Caringal Y.V., Dally R., Johnson J.S., Katz M.E., Kennure N., Kingery-Wood J.et al. Discovery of heterocyclic ureas as a new class of Raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach. Bioorg. Med. Chem. Lett. 11:2001;2775-2778.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2775-2778
-
-
Smith, R.A.1
Barbosa, J.2
Blum, C.L.3
Bobko, M.A.4
Caringal, Y.V.5
Dally, R.6
Johnson, J.S.7
Katz, M.E.8
Kennure, N.9
Kingery-Wood, J.10
-
61
-
-
0035086636
-
The discovery of RPR-200765, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy
-
Successful application of project-driven libraries. Clinical candidate identified
-
Mclay L.M., Halley F., Souness J.E., McKenna J., Benning V., Birrell M., Burton B., Belvisi M., Collis A., Constan A.et al. The discovery of RPR-200765, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy. Bioorg. Med. Chem. Lett. 11:2001;537-554 Successful application of project-driven libraries. Clinical candidate identified.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 537-554
-
-
Mclay, L.M.1
Halley, F.2
Souness, J.E.3
McKenna, J.4
Benning, V.5
Birrell, M.6
Burton, B.7
Belvisi, M.8
Collis, A.9
Constan, A.10
-
62
-
-
0037161596
-
An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors
-
McKenna J.M., Halley F., Souness J.E., McLay I.M., Pickett S.D., Collis A.J., Page K., Ahmed I. An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors. J. Med. Chem. 45:2002;2173-2184.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2173-2184
-
-
McKenna, J.M.1
Halley, F.2
Souness, J.E.3
McLay, I.M.4
Pickett, S.D.5
Collis, A.J.6
Page, K.7
Ahmed, I.8
-
63
-
-
0035820526
-
Phenoxypyrimidine inhibitors of p38a kinase: Synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles
-
Boehm J.C., Bower M.J., Gallagher T.F., Kassis S., Johnson S.R., Adams J.L. Phenoxypyrimidine inhibitors of p38a kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles. Bioorg. Med. Chem. Lett. 11:2001;1123-1126.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1123-1126
-
-
Boehm, J.C.1
Bower, M.J.2
Gallagher, T.F.3
Kassis, S.4
Johnson, S.R.5
Adams, J.L.6
-
64
-
-
18644368173
-
Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: A new class of KDR kinase inhibitors
-
Fraley M.E., Hoffman W.F., Rubino R.S., Hungate R.W., Tebben A.J., Rutledge R.Z., McFall R.C., Huckle W.R., Kendall R.L., Coll K.E., Thomas K.A. Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors. Bioorg. Med. Chem. Lett. 12:2002;2767-2770.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2767-2770
-
-
Fraley, M.E.1
Hoffman, W.F.2
Rubino, R.S.3
Hungate, R.W.4
Tebben, A.J.5
Rutledge, R.Z.6
McFall, R.C.7
Huckle, W.R.8
Kendall, R.L.9
Coll, K.E.10
Thomas, K.A.11
-
65
-
-
18344373265
-
Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56Lck
-
Chen P., Norris D., Iwanowicz E.J., Spergel S.H., Lin J., Gu H.H., Shen Z., Wityak J., Lin T.A., Pang S.et al. Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56Lck. Bioorg. Med. Chem. Lett. 12:2002;1361-1364.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1361-1364
-
-
Chen, P.1
Norris, D.2
Iwanowicz, E.J.3
Spergel, S.H.4
Lin, J.5
Gu, H.H.6
Shen, Z.7
Wityak, J.8
Lin, T.A.9
Pang, S.10
-
66
-
-
0035825362
-
Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors
-
Cowart M., Lee C.H., Gfesser G.A., Bayburt E.K., Bhagwat S.S., Stewart A.O., Yu H., Kohlhaas K.L., McGaraughty S., Wismer C.T.et al. Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors. Bioorg. Med. Chem. Lett. 11:2001;83-86.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 83-86
-
-
Cowart, M.1
Lee, C.H.2
Gfesser, G.A.3
Bayburt, E.K.4
Bhagwat, S.S.5
Stewart, A.O.6
Yu, H.7
Kohlhaas, K.L.8
McGaraughty, S.9
Wismer, C.T.10
-
67
-
-
17944366392
-
Pyridopyrimidines analogues as novel adenosine kinase inhibitors
-
Zheng G.Z.et al. Pyridopyrimidines analogues as novel adenosine kinase inhibitors. Bioorg. Med. Chem. Lett. 11:2001;2071-2074.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2071-2074
-
-
Zheng, G.Z.1
-
68
-
-
0037186459
-
Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1)
-
Callahan J.F., Burgess J.L., Fornwald J.A., Gaster L.M., Harling J.D., Harrington F.P., Heer J., Kwon C., Lehr R., Mathur A.et al. Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1). J. Med. Chem. 45:2002;999-1001.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 999-1001
-
-
Callahan, J.F.1
Burgess, J.L.2
Fornwald, J.A.3
Gaster, L.M.4
Harling, J.D.5
Harrington, F.P.6
Heer, J.7
Kwon, C.8
Lehr, R.9
Mathur, A.10
-
69
-
-
0037124187
-
Synthesis and bioactivities of novel 4,5,6,7-tetrahydothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-α (TNF-α) production
-
Fujita M., Seki T., Inada H., Ikeda N. Synthesis and bioactivities of novel 4,5,6,7-tetrahydothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-α (TNF-α) production. Bioorg. Med. Chem. Lett. 12:2002;1607-1611.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1607-1611
-
-
Fujita, M.1
Seki, T.2
Inada, H.3
Ikeda, N.4
-
70
-
-
0037026184
-
Synthesis and PTP1B inhibition of 1,2-naphtoquinone derivatives as potent anti-diabetic agents
-
Ahn J.H., Cho S.Y., Ha J.D., Chu S.Y., Jung S.H., Jung Y.S., Baek J.Y., Choi I.K., Shin E.Y., Kang S.K.et al. Synthesis and PTP1B inhibition of 1,2-naphtoquinone derivatives as potent anti-diabetic agents. Bioorg. Med. Chem. Lett. 12:2002;1941-1946.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1941-1946
-
-
Ahn, J.H.1
Cho, S.Y.2
Ha, J.D.3
Chu, S.Y.4
Jung, S.H.5
Jung, Y.S.6
Baek, J.Y.7
Choi, I.K.8
Shin, E.Y.9
Kang, S.K.10
-
71
-
-
0037194619
-
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: Synthesis, X-ray crystallographic analysis, and biological activities
-
Kim K.S., Kimball S.D., Misra R.N., Rawlins D.B., Hunt J.T., Xiao H.Y., Lu S., Qian L., Han W.C., Shan W.et al. Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. J. Med. Chem. 45:2002;3905-3927.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 3905-3927
-
-
Kim, K.S.1
Kimball, S.D.2
Misra, R.N.3
Rawlins, D.B.4
Hunt, J.T.5
Xiao, H.Y.6
Lu, S.7
Qian, L.8
Han, W.C.9
Shan, W.10
-
72
-
-
0035848403
-
3-Anilino-4-arylmaleimides: Potent and selective inhibitors of glycogen synthase kinase (GSK-3)
-
Smith D.G., Buffet M., Fenwick A.E., Haigh D., Ife R.J., Saunders M., Slingsby B.P., Stacey R., Ward R.W. 3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase (GSK-3). Bioorg. Med. Chem. Lett. 11:2001;635-639.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 635-639
-
-
Smith, D.G.1
Buffet, M.2
Fenwick, A.E.3
Haigh, D.4
Ife, R.J.5
Saunders, M.6
Slingsby, B.P.7
Stacey, R.8
Ward, R.W.9
-
73
-
-
17944365931
-
Substituted imidazoles as glucagon receptor antagonists
-
Chang L.L., Sidler K.L., Cascieri M.A., de Laszlo S., Koch G., Li B., MacCoss M., Mantlo N., O'Keefe S., Pang M.et al. Substituted imidazoles as glucagon receptor antagonists. Bioorg. Med. Chem. Lett. 11:2001;2549-2553.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2549-2553
-
-
Chang, L.L.1
Sidler, K.L.2
Cascieri, M.A.3
De Laszlo, S.4
Koch, G.5
Li, B.6
MacCoss, M.7
Mantlo, N.8
O'Keefe, S.9
Pang, M.10
-
74
-
-
0035855876
-
Identification of alkylidene hydrazides as glucagon receptor antagonist
-
Ling A., Hong Y., Gonzalez J., Gregor V., Polinsky A., Kuki A., Shi S., Teston K., Murphy D., Porter J.et al. Identification of alkylidene hydrazides as glucagon receptor antagonist. J. Med. Chem. 44:2001;3141-3149.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 3141-3149
-
-
Ling, A.1
Hong, Y.2
Gonzalez, J.3
Gregor, V.4
Polinsky, A.5
Kuki, A.6
Shi, S.7
Teston, K.8
Murphy, D.9
Porter, J.10
-
75
-
-
0037059908
-
Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists
-
Ladouceur G.H., Cook J.H., Doherty E.M., Schoen W.R., MacDougall M.L., Livingston J.N. Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists. Bioorg. Med. Chem. Lett. 12:2002;461-464.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 461-464
-
-
Ladouceur, G.H.1
Cook, J.H.2
Doherty, E.M.3
Schoen, W.R.4
MacDougall, M.L.5
Livingston, J.N.6
-
76
-
-
18344379308
-
Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: Development of an efficient, alternative synthesis
-
Smith R.A., Hertzog D.L., Osterhout M.H., Ladouceur G.H., Korpusik M., Bobko M.A., Jones J.H., Phelan K., Romero R.H., Hundertmark T.et al. Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: development of an efficient, alternative synthesis. Bioorg. Med. Chem. Lett. 12:2002;1303-1306.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1303-1306
-
-
Smith, R.A.1
Hertzog, D.L.2
Osterhout, M.H.3
Ladouceur, G.H.4
Korpusik, M.5
Bobko, M.A.6
Jones, J.H.7
Phelan, K.8
Romero, R.H.9
Hundertmark, T.10
-
77
-
-
0037578334
-
Discovery of a potent, orally active and clinically efficacious MTP inhibitor via a high-speed synthesis paradigm
-
Chang G et al.: Discovery of a Potent, Orally Active and Clinically Efficacious MTP Inhibitor via a High-speed Synthesis Paradigm. XIV International Symposium on Drugs AffectingLipid Metabolism, New York, NY, USA (2001):113.
-
(2001)
XIV International Symposium on Drugs AffectingLipid Metabolism, New York, NY, USA
, pp. 113
-
-
Chang, G.1
-
78
-
-
0036653640
-
Microsomal triglyceride transfer protein (MTP) inhibitors: Discovery of clinically active inhibitors using high-throughput screening and parallel synthesis paradigms
-
A successful application of HTS and combinatorial chemistry in the drug-discovery process. Clinical candidate identified
-
Chang G., Ruggeri R.B., Harwood J. Jr. Microsomal triglyceride transfer protein (MTP) inhibitors: discovery of clinically active inhibitors using high-throughput screening and parallel synthesis paradigms. Curr. Opin. Drug Discov. Dev. 5:2002;562-570 A successful application of HTS and combinatorial chemistry in the drug-discovery process. Clinical candidate identified.
-
(2002)
Curr. Opin. Drug Discov. Dev.
, vol.5
, pp. 562-570
-
-
Chang, G.1
Ruggeri, R.B.2
Harwood J., Jr.3
-
79
-
-
0035803032
-
Beta 3 agonists. Part 1: Evolution from inception to BMS-194449
-
Washburn W.N., Sher P.M., Poss K.M., Girotra R.N., McCann P.J., Gavai A.V., Mikkilineni A.B., Mathur A., Cheng P., Dejneka T.C.et al. Beta 3 agonists. Part 1: evolution from inception to BMS-194449. Bioorg. Med. Chem. Lett. 11:2001;3035-3039.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 3035-3039
-
-
Washburn, W.N.1
Sher, P.M.2
Poss, K.M.3
Girotra, R.N.4
McCann, P.J.5
Gavai, A.V.6
Mikkilineni, A.B.7
Mathur, A.8
Cheng, P.9
Dejneka, T.C.10
-
80
-
-
0035802971
-
BMS-196085: A potent and selective full agonist of the human β3 adrenergic receptor
-
Clinical candidate discovered
-
Gavai A.V., Sher P.M., Mikkilineni A.B., Poss K.M., McCann P.J., Girotra R.N., Fisher L.G., Wu G., Bednarz M.S., Mathur A.et al. BMS-196085: a potent and selective full agonist of the human β3 adrenergic receptor. Bioorg. Med. Chem. Lett. 11:2001;3041-3044 Clinical candidate discovered.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 3041-3044
-
-
Gavai, A.V.1
Sher, P.M.2
Mikkilineni, A.B.3
Poss, K.M.4
McCann, P.J.5
Girotra, R.N.6
Fisher, L.G.7
Wu, G.8
Bednarz, M.S.9
Mathur, A.10
-
81
-
-
0037161585
-
2-(Anilinomethyl)imidazolines as α1 adrenergic receptor agonists: The discovery of a1a subtype selective 2′-alkylsulfonyl-substituted analogues
-
Hodson S.J.et al. 2-(Anilinomethyl)imidazolines as α1 adrenergic receptor agonists: the discovery of a1a subtype selective 2′-alkylsulfonyl-substituted analogues. J. Med. Chem. 45:2002;2229-2239.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2229-2239
-
-
Hodson, S.J.1
-
82
-
-
0037042780
-
CCR3 Antagonists: A potential new therapy for the treatment of asthma. Discovery and structure-activity relationships
-
Wacker D.A., Santella J.B., Gardner D.S., Varnes J.G., Estrella M., DeLucca G.V., Ko S.S., Tanabe K., Watson P.S., Welch P.K.et al. CCR3 Antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships. Bioorg. Med. Chem. Lett. 12:2002;1785-1789.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1785-1789
-
-
Wacker, D.A.1
Santella, J.B.2
Gardner, D.S.3
Varnes, J.G.4
Estrella, M.5
DeLucca, G.V.6
Ko, S.S.7
Tanabe, K.8
Watson, P.S.9
Welch, P.K.10
-
83
-
-
0037103267
-
Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperedines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists
-
De Lucca G.V., Kim U.T., Johnson C., Vargo B.J., Welch P.K., Covington M., Davies P., Solomon K.A., Newton R.C., Trainor G.L.et al. Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperedines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists. J. Med. Chem. 45:2002;3794-3804.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 3794-3804
-
-
De Lucca, G.V.1
Kim, U.T.2
Johnson, C.3
Vargo, B.J.4
Welch, P.K.5
Covington, M.6
Davies, P.7
Solomon, K.A.8
Newton, R.C.9
Trainor, G.L.10
-
84
-
-
0035921055
-
Piperazine based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element
-
Tagat J.R., Steensma R.W., McCombie S.W., Nazareno D.V., Lin S.I., Neustadt B.R., Cox K., Xu S., Wojcik L., Murray M.G.et al. Piperazine based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element. Bioorg. Med. Chem. Lett. 11:2001;2143-2146.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2143-2146
-
-
Tagat, J.R.1
Steensma, R.W.2
McCombie, S.W.3
Nazareno, D.V.4
Lin, S.I.5
Neustadt, B.R.6
Cox, K.7
Xu, S.8
Wojcik, L.9
Murray, M.G.10
-
85
-
-
0035846074
-
Discovery of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1′-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4′-methyl-1,4′-bipiperidine N-oxide (1): An orally bioavailable human CCR5 antagonist for treatment of HIV infection
-
Palani A., Shapiro S., Clader J.W., Greenlee W.J., Cox K., Strizki J., Endres M., Baroudy B.M. Discovery of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1′-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4′-methyl-1,4′-bipiperidine N-oxide (1): An orally bioavailable human CCR5 antagonist for treatment of HIV infection. J. Med. Chem. 44:2001;3339-3342.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 3339-3342
-
-
Palani, A.1
Shapiro, S.2
Clader, J.W.3
Greenlee, W.J.4
Cox, K.5
Strizki, J.6
Endres, M.7
Baroudy, B.M.8
-
86
-
-
0037019271
-
Synthesis, SAR and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity
-
Palani A., Shapiro S., Josien H., Bara T., Clader J.W., Greenlee W.J., Cox K., Strizki J.M., Baroudy B.M. Synthesis, SAR and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity. J. Med. Chem. 45:2002;3143-3160.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 3143-3160
-
-
Palani, A.1
Shapiro, S.2
Josien, H.3
Bara, T.4
Clader, J.W.5
Greenlee, W.J.6
Cox, K.7
Strizki, J.M.8
Baroudy, B.M.9
-
87
-
-
0035931442
-
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationship for 1-amino-2-phenyl-4-(piperdin-1-yl)butanes
-
Dorn C.P., Finke P.E., Oates B., Budhu R.J., Mills S.G., MacCoss M., Malkowitz L., Springer M.S., Daugherty B.L., Gould S.L.et al. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationship for 1-amino-2-phenyl-4-(piperdin-1-yl)butanes. Bioorg. Med. Chem. Lett. 11:2001;259-264.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 259-264
-
-
Dorn, C.P.1
Finke, P.E.2
Oates, B.3
Budhu, R.J.4
Mills, S.G.5
MacCoss, M.6
Malkowitz, L.7
Springer, M.S.8
Daugherty, B.L.9
Gould, S.L.10
-
88
-
-
0035931392
-
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationship for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes
-
Finke P.E., Meurer L.C., Oates B., Mills S.G., MacCoss M., Malkowitz L., Springer M.S., Daugherty B.L., Gould S.L., DeMartino J.A.et al. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationship for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. 11:2001;265-270.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 265-270
-
-
Finke, P.E.1
Meurer, L.C.2
Oates, B.3
Mills, S.G.4
MacCoss, M.5
Malkowitz, L.6
Springer, M.S.7
Daugherty, B.L.8
Gould, S.L.9
DeMartino, J.A.10
-
89
-
-
0035806039
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: Discovery of the pyrrolidine scaffold and determination of its stereochemical requirements
-
Hale J.J., Budhu R.J., Mills S.G., MacCoss M., Gould S.L., DeMartino J.A., Springer M.S., Siciliano S.J., Malkowitz L., Schleif W.A.et al. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: Discovery of the pyrrolidine scaffold and determination of its stereochemical requirements. Bioorg. Med. Chem. Lett. 11:2001;1437-1440.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1437-1440
-
-
Hale, J.J.1
Budhu, R.J.2
Mills, S.G.3
MacCoss, M.4
Gould, S.L.5
DeMartino, J.A.6
Springer, M.S.7
Siciliano, S.J.8
Malkowitz, L.9
Schleif, W.A.10
-
90
-
-
0035935205
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: Lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity
-
Hale J.J., Budhu R.J., Holson E.B., Finke P.E., Oates B., Mills S.G., MacCoss M., Gould S.L., DeMartino J.A., Springer M.S.et al. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: Lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity. Bioorg. Med. Chem. Lett. 11:2001;2741-2745.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2741-2745
-
-
Hale, J.J.1
Budhu, R.J.2
Holson, E.B.3
Finke, P.E.4
Oates, B.5
Mills, S.G.6
MacCoss, M.7
Gould, S.L.8
DeMartino, J.A.9
Springer, M.S.10
-
91
-
-
0035904882
-
Combinatorial synthesis of CCR5 antagonists
-
An excellent example of thematic library design and synthesis, successful for multiple biological targets
-
Willoughby C.A., Berk S.C., Rosauer K.G., Degrado S., Chapman K.T., Gould S.L., Springer M.S., Malkowitz L., Schleif W.A., Hazuda D.et al. Combinatorial synthesis of CCR5 antagonists. Bioorg. Med. Chem. Lett. 11:2001;3137-3141 An excellent example of thematic library design and synthesis, successful for multiple biological targets.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 3137-3141
-
-
Willoughby, C.A.1
Berk, S.C.2
Rosauer, K.G.3
Degrado, S.4
Chapman, K.T.5
Gould, S.L.6
Springer, M.S.7
Malkowitz, L.8
Schleif, W.A.9
Hazuda, D.10
-
92
-
-
0035952261
-
Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles
-
Chu L., Hutchins J.E., Weber A.E., Lo J.L., Yang Y.T., Cheng K., Smith R.G., Fisher M.H., Wyvratt M.J., Goulet M.T. Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles. Bioorg. Med. Chem. Lett. 11:2001;509-513.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 509-513
-
-
Chu, L.1
Hutchins, J.E.2
Weber, A.E.3
Lo, J.L.4
Yang, Y.T.5
Cheng, K.6
Smith, R.G.7
Fisher, M.H.8
Wyvratt, M.J.9
Goulet, M.T.10
-
93
-
-
0035952296
-
SAR Studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists
-
Chu L., Lo J.L., Yang Y.T., Cheng K., Smith R.G., Fisher M.H., Wyvratt M.J., Goulet M.T. SAR Studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists. Bioorg. Med. Chem. Lett. 11:2001;515-517.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 515-517
-
-
Chu, L.1
Lo, J.L.2
Yang, Y.T.3
Cheng, K.4
Smith, R.G.5
Fisher, M.H.6
Wyvratt, M.J.7
Goulet, M.T.8
-
94
-
-
0035833079
-
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists
-
Ashton W.T., Sisco R.M., Yang Y.T., Lo J.L., Yudkovitz J.B., Cheng K., Goulet M.T. Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists. Bioorg. Med. Chem. Lett. 11:2001;1723-1726.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1723-1726
-
-
Ashton, W.T.1
Sisco, R.M.2
Yang, Y.T.3
Lo, J.L.4
Yudkovitz, J.B.5
Cheng, K.6
Goulet, M.T.7
-
95
-
-
0035833079
-
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists
-
Ashton W.T., Sisco R.M., Yang Y.T., Yang Y.T., Lo J.L., Yudkovitz A., Gibbons P.H., Mount G.R., Ren R.N., Butler B.S.et al. Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists. Bioorg. Med. Chem. Lett. 11:2001;1727-1731.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1727-1731
-
-
Ashton, W.T.1
Sisco, R.M.2
Yang, Y.T.3
Yang, Y.T.4
Lo, J.L.5
Yudkovitz, A.6
Gibbons, P.H.7
Mount, G.R.8
Ren, R.N.9
Butler, B.S.10
-
96
-
-
17944383430
-
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity
-
Ashton W.T., Sisco R.M., Kieczykowski G.R., Yang Y.T., Yudkovitz J.B., Cui J., Mount G.R., Ren R.N., Wu T.J., Shen X.et al. Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity. Bioorg. Med. Chem. Lett. 11:2001;2597-2602.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2597-2602
-
-
Ashton, W.T.1
Sisco, R.M.2
Kieczykowski, G.R.3
Yang, Y.T.4
Yudkovitz, J.B.5
Cui, J.6
Mount, G.R.7
Ren, R.N.8
Wu, T.J.9
Shen, X.10
-
97
-
-
0035866652
-
A potent, nonpeptidyl 1-H-quinolone antagonist for the gonadotropin-releasing hormone receptor
-
DeVita R.J., Walsh T.F., Young J.R., Jiang J., Ujjainwalla F., Toupence R.B., Parikh M., Huang S.X., Fair J.A., Goulet M.T.et al. A potent, nonpeptidyl 1-H-quinolone antagonist for the gonadotropin-releasing hormone receptor. J. Med. Chem. 44:2001;917-922.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 917-922
-
-
DeVita, R.J.1
Walsh, T.F.2
Young, J.R.3
Jiang, J.4
Ujjainwalla, F.5
Toupence, R.B.6
Parikh, M.7
Huang, S.X.8
Fair, J.A.9
Goulet, M.T.10
-
98
-
-
18244382828
-
Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: Discovery of potent ligands for a variety of G-coupled receptors
-
••] An excellent example of thematic library design and synthesis, successful for multiple biological targets
-
••] An excellent example of thematic library design and synthesis, successful for multiple biological targets.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 93-96
-
-
Willoughby, C.A.1
Hutchins, S.M.2
Rosauer, K.G.3
Dhar, M.J.4
Chapman, K.T.5
Chicchi, G.G.6
Sadowski, S.7
Weinberg, D.H.8
Patel, S.9
Malkowitz, L.10
-
99
-
-
0035821395
-
1 receptor antagonists: Optimization of indole substitution
-
1 receptor antagonists: optimization of indole substitution. Bioorg. Med. Chem. Lett. 11:2001;1233-1236.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1233-1236
-
-
Cooper, L.C.1
Chicchi, G.G.2
Dinnell, K.3
Elliott, J.M.4
Hollingworth, G.J.5
Kurtz, M.M.6
Locker, K.L.7
Morrison, D.8
Shaw, D.E.9
Tsao, K.L.10
-
100
-
-
0035821416
-
1 receptor antagonists: Optimization of the 2-aryl ring and the indole nitrogen substituent
-
1 receptor antagonists: optimization of the 2-aryl ring and the indole nitrogen substituent. Bioorg. Med. Chem. Lett. 11:2001;1237-1240.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1237-1240
-
-
Dinnell, K.1
Chicchi, G.G.2
Dhar, M.J.3
Elliott, J.M.4
Hollingworth, G.J.5
Kurtz, M.M.6
Ridgill, M.P.7
Rycroft, W.8
Tsao, K.L.9
Williams, A.R.10
Swain, C.J.11
-
101
-
-
0035802986
-
1 antagonists: Optimization of the amide substituent
-
1 antagonists: optimization of the amide substituent. Bioorg. Med. Chem. Lett. 11:2001;3031-3034.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 3031-3034
-
-
Shaw, A.1
-
102
-
-
0035833030
-
Expedited discovery of second generation NK-1 antagonists: Identification of a nonbasic aryloxy substituent
-
Fritz J.E., Hipskind P.A., Lobb K.L., Nixon J.A., Threlkeld P.G., Gitter B.D., McMillian C.L., Kador S.W. Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent. Bioorg. Med. Chem. Lett. 11:2001;1643-1646.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1643-1646
-
-
Fritz, J.E.1
Hipskind, P.A.2
Lobb, K.L.3
Nixon, J.A.4
Threlkeld, P.G.5
Gitter, B.D.6
McMillian, C.L.7
Kador, S.W.8
-
103
-
-
18244393222
-
1 receptor antagonists
-
1 receptor antagonists. Bioorg. Med. Chem. Lett. 12:2002;379-382.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 379-382
-
-
Poindexter, G.S.1
Bruce, M.A.2
LeBoulluec, K.L.3
Monkovic, I.4
Martin, S.W.5
Parker, E.M.6
Iben, L.G.7
McGovern, R.T.8
Ortiz, A.A.9
Stanley, J.A.10
-
104
-
-
0035801757
-
Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor
-
Kordik C.P., Luo C., Zanoni B.C., Dax S.L., McNally J.J., Lovenberg T.W., Wilson S.J., Reitz A.B. Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor. Bioorg. Med. Chem. Lett. 11:2001;2283-2286.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2283-2286
-
-
Kordik, C.P.1
Luo, C.2
Zanoni, B.C.3
Dax, S.L.4
McNally, J.J.5
Lovenberg, T.W.6
Wilson, S.J.7
Reitz, A.B.8
-
105
-
-
0035801739
-
Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity
-
Kordik C.P., Luo C., Zanoni B.C., Lovenberg T.W., Wilson S.J., Vaidya A.H., Crooke J.J., Rosenthal D.I., Reitz A.B. Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity. Bioorg. Med. Chem. Lett. 11:2001;2287-2290.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2287-2290
-
-
Kordik, C.P.1
Luo, C.2
Zanoni, B.C.3
Lovenberg, T.W.4
Wilson, S.J.5
Vaidya, A.H.6
Crooke, J.J.7
Rosenthal, D.I.8
Reitz, A.B.9
-
106
-
-
0037156335
-
Novel potent antagonist of human neuropeptide Y Y5 receptor. Part 1: 2-oxobenzothiazolin-3-acetic acid derivatives
-
Tabuchi S., Itani H., Sakata Y., Oohashi H., Satoh Y. Novel potent antagonist of human neuropeptide Y Y5 receptor. Part 1: 2-oxobenzothiazolin-3-acetic acid derivatives. Bioorg. Med. Chem. Lett. 12:2002;1171-1175.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1171-1175
-
-
Tabuchi, S.1
Itani, H.2
Sakata, Y.3
Oohashi, H.4
Satoh, Y.5
-
107
-
-
0037041219
-
Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: Tetrahydrodiazabenzazulene derivatives
-
Satoh Y., Hatori C., Ito H. Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: Tetrahydrodiazabenzazulene derivatives. Bioorg. Med. Chem. Lett. 12:2002;1009-1011.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1009-1011
-
-
Satoh, Y.1
Hatori, C.2
Ito, H.3
-
108
-
-
0035811460
-
Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists
-
Fotsch C., Sonnenberg J.D., Chen N., Hale C., Karbon W., Norman M.H. Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists. J. Med. Chem. 44:2001;2344-2356.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2344-2356
-
-
Fotsch, C.1
Sonnenberg, J.D.2
Chen, N.3
Hale, C.4
Karbon, W.5
Norman, M.H.6
-
110
-
-
0037114945
-
Targeting signal transduction with large combinatorial collections
-
Auld D.S., Diller D., Ho K.-K. Targeting signal transduction with large combinatorial collections. Drug Discov Today. 7:2002;1206-1213.
-
(2002)
Drug Discov Today
, vol.7
, pp. 1206-1213
-
-
Auld, D.S.1
Diller, D.2
Ho, K.-K.3
-
111
-
-
85031145721
-
Discovery of a novel class of selective muscarinic M1 agonists suitable for clinical development
-
New Orleans, MEDI-330
-
Hitchcock S, Allen J, Baker A, Bensinger J, Bick P, Bymaster F, Delapp N, Gannon K, Gregory GS, Hansen M et al.: Discovery of a novel class of selective muscarinic M1 agonists suitable for clinical development. Abstract of Papers, 25th ACS National Meeting: 2003 March 23-272; New Orleans, MEDI-330.
-
Abstract of Papers, 25th ACS National Meeting: 2003 March 23-272
-
-
Hitchcock, S.1
Allen, J.2
Baker, A.3
Bensinger, J.4
Bick, P.5
Bymaster, F.6
Delapp, N.7
Gannon, K.8
Gregory, G.S.9
Hansen, M.10
-
112
-
-
85031161461
-
Discovery of potent, selective, and orally active CCR5 antagonists for the potential treatment of HIV infection
-
New Orleans, MEDI-015
-
Jayaram T, McCombie S, Nazareno D, Steensma R, Labroli M, Baroudy B, Strizki J, Cox K: Discovery of potent, selective, and orally active CCR5 antagonists for the potential treatment of HIV infection. Abstract of Papers, 25th ACS National Meeting: 2003 March 23-272; New Orleans, MEDI-015.
-
Abstract of Papers, 25th ACS National Meeting: 2003 March 23-272
-
-
Jayaram, T.1
McCombie, S.2
Nazareno, D.3
Steensma, R.4
Labroli, M.5
Baroudy, B.6
Strizki, J.7
Cox, K.8
|