-
2
-
-
0032589679
-
Severe anemia as a newly recognized side-effect caused by lamivudine
-
Weitzel, T.; Plettenberg, A.; Albrecht, D.; Lorenzen, T.; Stoehr, A. Severe anemia as a newly recognized side-effect caused by lamivudine. AIDS 1999, 13, 2309-2311.
-
(1999)
AIDS
, vol.13
, pp. 2309-2311
-
-
Weitzel, T.1
Plettenberg, A.2
Albrecht, D.3
Lorenzen, T.4
Stoehr, A.5
-
3
-
-
0034057091
-
Rash as side-effect of nelfinavir in children
-
Fortuny, C.; Vicente, M. A.; Medina, M. M.; Gonzalez-Ensenat, A. Rash as side-effect of nelfinavir in children. AIDS 2000, 14, 335-336.
-
(2000)
AIDS
, vol.14
, pp. 335-336
-
-
Fortuny, C.1
Vicente, M.A.2
Medina, M.M.3
Gonzalez-Ensenat, A.4
-
4
-
-
0033786335
-
Keratinocyte growth factor is upregulated by the hyperplasia-inducing drug nifedipine
-
Das, S. J.; Olsen, I. Keratinocyte growth factor is upregulated by the hyperplasia-inducing drug nifedipine. Cytokine 2000, 12, 1566-1569.
-
(2000)
Cytokine
, vol.12
, pp. 1566-1569
-
-
Das, S.J.1
Olsen, I.2
-
5
-
-
0035345717
-
Evidence of hypertriglyceridemia in managing HIV patients on efavirenz
-
Savini, C. J.; James, C. W.; Miller, J. L.; Wilson, S. A.; Cohen, D. M.; Perlada, D. E. Evidence of hypertriglyceridemia in managing HIV patients on efavirenz. J. Assoc. Nurses AIDS Care 2001, 12, 95-97.
-
(2001)
J. Assoc. Nurses AIDS Care
, vol.12
, pp. 95-97
-
-
Savini, C.J.1
James, C.W.2
Miller, J.L.3
Wilson, S.A.4
Cohen, D.M.5
Perlada, D.E.6
-
6
-
-
0035823019
-
Direct analysis of mitochondrial toxicity of antiretroviral drugs
-
Foli, A.; Benvenuto, F.; Piccinini, G.; Bareggi, A.; Cossarizza, A.; Lisziewicz, J.; Lori, F. Direct analysis of mitochondrial toxicity of antiretroviral drugs. AIDS 2001, 15, 1687-1694.
-
(2001)
AIDS
, vol.15
, pp. 1687-1694
-
-
Foli, A.1
Benvenuto, F.2
Piccinini, G.3
Bareggi, A.4
Cossarizza, A.5
Lisziewicz, J.6
Lori, F.7
-
7
-
-
0036462258
-
Resistance profiles of cyclic and linear inhibitors of HIV-1 protease
-
Ahlsen, G.; Hulten, J.; Shuman, C. F.; Poliakov, A.; Lindgren, M. T.; Alterman, M.; Samuelsson, B.; Hallberg, A.; Danielson, U. H. Resistance profiles of cyclic and linear inhibitors of HIV-1 protease. Antiviral Chem. Chemother. 2002, 13, 27-37.
-
(2002)
Antiviral Chem. Chemother.
, vol.13
, pp. 27-37
-
-
Ahlsen, G.1
Hulten, J.2
Shuman, C.F.3
Poliakov, A.4
Lindgren, M.T.5
Alterman, M.6
Samuelsson, B.7
Hallberg, A.8
Danielson, U.H.9
-
8
-
-
0036629894
-
HIV resistance to antiretroviral drugs: Mechanisms, genotypic and phenotypic resistance testing in clinical practice
-
Blaise, P.; Clevenbergh, P.; Vaira, D.; Moutschen, M.; Dellamonica, P. HIV resistance to antiretroviral drugs: mechanisms, genotypic and phenotypic resistance testing in clinical practice. Acta Clin. Belg. 2002, 57, 191-201.
-
(2002)
Acta Clin. Belg.
, vol.57
, pp. 191-201
-
-
Blaise, P.1
Clevenbergh, P.2
Vaira, D.3
Moutschen, M.4
Dellamonica, P.5
-
9
-
-
0038389095
-
Resistance to protease inhibitors
-
Kuritzkes, D. R. Resistance to protease inhibitors. J. HIV Ther. 2002, 7, 87-91.
-
(2002)
J. HIV Ther.
, vol.7
, pp. 87-91
-
-
Kuritzkes, D.R.1
-
10
-
-
0035289055
-
Fusion inhibitors: T-20 and T-1249
-
Fusion inhibitors: T-20 and T-1249. Treatmentupdate 2001, 12, 2-3.
-
(2001)
Treatmentupdate
, vol.12
, pp. 2-3
-
-
-
11
-
-
0037502870
-
T-20: Most expensive AIDS drug ever at $25,000 per year?
-
James, J. S. T-20: most expensive AIDS drug ever at $25,000 per year? AIDS Treat. News 2003, 6-7.
-
(2003)
AIDS Treat. News
, pp. 6-7
-
-
James, J.S.1
-
12
-
-
0032600559
-
T-20: First of a new class of anti-HIV drugs
-
Hanna, L. T-20: first of a new class of anti-HIV drugs. BETA 1999, 12, 7-8.
-
(1999)
BETA
, vol.12
, pp. 7-8
-
-
Hanna, L.1
-
13
-
-
0038100552
-
FUZEON (enfuvirtide, T-20). Breaking barriers or breaking the bank?
-
Sharp, M.; Camp, R. FUZEON (enfuvirtide, T-20). Breaking barriers or breaking the bank? GMHC Treat. Issues 2003, 17, 7-8.
-
(2003)
GMHC Treat. Issues
, vol.17
, pp. 7-8
-
-
Sharp, M.1
Camp, R.2
-
14
-
-
0037320947
-
HIV-1 cell entry and advances in viral entry inhibitor therapy
-
Cooley, L. A.; Lewin, S. R. HIV-1 cell entry and advances in viral entry inhibitor therapy. J. Clin. Virol. 2003, 26, 121-132.
-
(2003)
J. Clin. Virol.
, vol.26
, pp. 121-132
-
-
Cooley, L.A.1
Lewin, S.R.2
-
15
-
-
0345700287
-
Entry inhibitors SCH-C, RANTES T-20 block HIV type 1 replication in multiple cell types
-
Ketas, T. J.; Klasse, P. J.; Spenlehauer, C.; Nesin, M.; Frank, I.; Pope, M.; Strizki, J. M.; Reyes, G. R.; Baroudy, B. M.; Moore, J. P. Entry Inhibitors SCH-C, RANTES, and T-20 Block HIV Type 1 Replication in Multiple Cell Types. AIDS Res. Hum. Retroviruses 2003, 19, 177-186.
-
(2003)
AIDS Res. Hum. Retroviruses
, vol.19
, pp. 177-186
-
-
Ketas, T.J.1
Klasse, P.J.2
Spenlehauer, C.3
Nesin, M.4
Frank, I.5
Pope, M.6
Strizki, J.M.7
Reyes, G.R.8
Baroudy, B.M.9
Moore, J.P.10
-
16
-
-
0037039380
-
HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use
-
Trkola, A.; Kuhmann, S. E.; Strizki, J. M.; Maxwell, E.; Ketas, T.; Morgan, T.; Pugach, P.; Xu, S.; Wojcik, L.; Tagat, J.; Palani, A.; Shapiro, S.; Clader, J. W.; McCombie, S.; Reyes, G. R.; Baroudy, B. M.; Moore, J. P. HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use. Proc. Natl. Acad. Sci. U.S.A. 2002, 99, 395-400.
-
(2002)
Proc. Natl. Acad. Sci. U.S.A.
, vol.99
, pp. 395-400
-
-
Trkola, A.1
Kuhmann, S.E.2
Strizki, J.M.3
Maxwell, E.4
Ketas, T.5
Morgan, T.6
Pugach, P.7
Xu, S.8
Wojcik, L.9
Tagat, J.10
Palani, A.11
Shapiro, S.12
Clader, J.W.13
McCombie, S.14
Reyes, G.R.15
Baroudy, B.M.16
Moore, J.P.17
-
17
-
-
0035663233
-
HIV-1 entry and how to block it
-
Brelot, A.; Alizon, M. HIV-1 entry and how to block it. AIDS 2001, 15 (Suppl. 5), S3-S11.
-
(2001)
AIDS
, vol.15
, Issue.SUPPL. 5
-
-
Brelot, A.1
Alizon, M.2
-
18
-
-
0030793861
-
Co-receptors for HIV-1 entry
-
Moore, J. P.; Trkola, A.; Dragic, T. Co-receptors for HIV-1 entry. Curr Opin. Immunol. 1997, 9, 551-562.
-
(1997)
Curr Opin. Immunol.
, vol.9
, pp. 551-562
-
-
Moore, J.P.1
Trkola, A.2
Dragic, T.3
-
19
-
-
0033615735
-
HIV-1 entry inhibitors in the side pocket
-
Sodroski, J. G. HIV-1 entry inhibitors in the side pocket. Cell 1999, 99, 243-246.
-
(1999)
Cell
, vol.99
, pp. 243-246
-
-
Sodroski, J.G.1
-
20
-
-
0026088207
-
Mechanism of HIV-1 entry into CD4+ T cells
-
Stein, B. S.; Engleman, E. G. Mechanism of HIV-1 entry into CD4+ T cells. Adv. Exp. Med. Biol. 1991, 300, 71-86.
-
(1991)
Adv. Exp. Med. Biol.
, vol.300
, pp. 71-86
-
-
Stein, B.S.1
Engleman, E.G.2
-
21
-
-
0029417004
-
Identification of RANTES, MIP-1 alpha, and MIP-1 beta as the major HIV-suppressive factors produced by CD8+ T cells
-
Cocchi, F.; DeVico, A. L.; Garzino-Demo, A.; Arya, S. K.; Gallo, R. C.; Lusso, P. Identification of RANTES, MIP-1 alpha, and MIP-1 beta as the major HIV-suppressive factors produced by CD8+ T cells. Science 1995, 270, 1811-1815.
-
(1995)
Science
, vol.270
, pp. 1811-1815
-
-
Cocchi, F.1
DeVico, A.L.2
Garzino-Demo, A.3
Arya, S.K.4
Gallo, R.C.5
Lusso, P.6
-
22
-
-
15844388931
-
Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection
-
Liu, R.; Paxton, W. A.; Choe, S.; Ceradini, D.; Martin, S. R.; Horuk, R. ; MacDonald, M. E.; Stuhlmann, H.; Koup, R. A.; Landau, N. R. Homozygous defect in HIV-1 coreceptor accounts for resistance of some multiply-exposed individuals to HIV-1 infection. Cell 1996, 86, 367-377.
-
(1996)
Cell
, vol.86
, pp. 367-377
-
-
Liu, R.1
Paxton, W.A.2
Choe, S.3
Ceradini, D.4
Martin, S.R.5
Horuk, R.6
MacDonald, M.E.7
Stuhlmann, H.8
Koup, R.A.9
Landau, N.R.10
-
23
-
-
0035881173
-
Homozygous and heterozygous CCR5-Delta32 genotypes are associated with resistance to HIV infection
-
Marmor, M.; Sheppard, H. W.; Donnell, D.; Bozeman, S.; Celum, C.; Buchbinder, S.; Koblin, B.; Seage, G. R., III. Homozygous and heterozygous CCR5-Delta32 genotypes are associated with resistance to HIV infection. J. Acquired Immune Defic. Syndr. 2001, 27, 472-481.
-
(2001)
J. Acquired Immune Defic. Syndr.
, vol.27
, pp. 472-481
-
-
Marmor, M.1
Sheppard, H.W.2
Donnell, D.3
Bozeman, S.4
Celum, C.5
Buchbinder, S.6
Koblin, B.7
Seage G.R. III8
-
24
-
-
16044373004
-
Resistance to HIV-1 infection in Caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene
-
Samson, M.; Libert, F.; Doranz, B. J.; Rucker, J.; Liesnard, C.; Farber, C. M.; Saragosti, S.; Lapoumeroulie, C.; Cognaux, J.; Forceille, C.; Muyldermans, G.; Verhofstede, C.; Burtonboy, G.; Georges, M.; Imai, T.; Rana, S.; Yi, Y.; Smyth, R. J.; Collman, R. G.; Doms, R. W.; Vassart, G.; Parmentier, M. Resistance to HIV-1 infection in Caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene. Nature 1996, 382, 722-725.
-
(1996)
Nature
, vol.382
, pp. 722-725
-
-
Samson, M.1
Libert, F.2
Doranz, B.J.3
Rucker, J.4
Liesnard, C.5
Farber, C.M.6
Saragosti, S.7
Lapoumeroulie, C.8
Cognaux, J.9
Forceille, C.10
Muyldermans, G.11
Verhofstede, C.12
Burtonboy, G.13
Georges, M.14
Imai, T.15
Rana, S.16
Yi, Y.17
Smyth, R.J.18
Collman, R.G.19
Doms, R.W.20
Vassart, G.21
Parmentier, M.22
more..
-
25
-
-
0037872129
-
Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors
-
Kazmierski, W.; Bifulco, N.; Yang, H.; Boone, L.; DeAnda, F.; Watson, C. ; Kenakin, T. Recent Progress in Discovery of Small-Molecule CCR5 Chemokine Receptor Ligands as HIV-1 Inhibitors. Bioorg. Med. Chem. 2003, 11, 2663-2667.
-
(2003)
Bioorg. Med. Chem.
, vol.11
, pp. 2663-2667
-
-
Kazmierski, W.1
Bifulco, N.2
Yang, H.3
Boone, L.4
DeAnda, F.5
Watson, C.6
Kenakin, T.7
-
26
-
-
13044256383
-
A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity
-
Baba, M.; Nishimura, O.; Kanzaki, N.; Okamoto, M.; Sawada, H.; Iizawa, Y.; Shiraishi, M.; Aramaki, Y.; Okonogi, K.; Ogawa, Y.; Meguro, K.; Fujino, M. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc. Natl. Acad. Sci. U.S.A. 1999, 96, 5698-5703.
-
(1999)
Proc. Natl. Acad. Sci. U.S.A.
, vol.96
, pp. 5698-5703
-
-
Baba, M.1
Nishimura, O.2
Kanzaki, N.3
Okamoto, M.4
Sawada, H.5
Iizawa, Y.6
Shiraishi, M.7
Aramaki, Y.8
Okonogi, K.9
Ogawa, Y.10
Meguro, K.11
Fujino, M.12
-
27
-
-
0035846074
-
Discovery of 4-[(Z)-(4-bromophenyl)-(ethoxyimino)methyl]-1′ -[(2,4-dimethyl-3-pyridinyl)carbonyl]-4′-methyl-1,4′-bipiperidine N-oxide (SCH 351125): An orally bioavailable human CCR5 antagonist for the 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 (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection. J. Med. Chem. 2001, 44, 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
-
28
-
-
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. 2002, 45, 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
-
29
-
-
0035940445
-
SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo
-
Strizki, J. M.; Xu, S.; Wagner, N. E.; Wojcik, L.; Liu, J.; Hou, Y.; Endres, M.; Palani, A.; Shapiro, S.; Clader, J. W.; Greenlee, W. J.; Tagat, J. R.; McCombie, S.; Cox, K.; Fawzi, A. B.; Chou, C. C.; Pugliese-Sivo, C.; Davies, L.; Moreno, M. E.; Ho, D. D.; Trkola, A.; Stoddart, C. A.; Moore, J. P.; Reyes, G. R.; Baroudy, B. M. SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo. Proc. Natl. Acad. Sci. U.S.A. 2001, 98, 12718-12723.
-
(2001)
Proc. Natl. Acad. Sci. U.S.A.
, vol.98
, pp. 12718-12723
-
-
Strizki, J.M.1
Xu, S.2
Wagner, N.E.3
Wojcik, L.4
Liu, J.5
Hou, Y.6
Endres, M.7
Palani, A.8
Shapiro, S.9
Clader, J.W.10
Greenlee, W.J.11
Tagat, J.R.12
McCombie, S.13
Cox, K.14
Fawzi, A.B.15
Chou, C.C.16
Pugliese-Sivo, C.17
Davies, L.18
Moreno, M.E.19
Ho, D.D.20
Trkola, A.21
Stoddart, C.A.22
Moore, J.P.23
Reyes, G.R.24
Baroudy, B.M.25
more..
-
30
-
-
0037404511
-
Analysis of the mechanism by which the small-molecule CCR5 antagonists SCH-351125 and SCH-350581 inhibit human immunodeficiency virus type 1 entry
-
Tsamis, F.; Gavrilov, S.; Kajumo, F.; Seibert, C.; Kuhmann, S.; Ketas, T.; Trkola, A.; Palani, A.; Clader, J. W.; Tagat, J. R.; McCombie, S.; Baroudy, B.; Moore, J. P.; Sakmar, T. P.; Dragic, T. Analysis of the mechanism by which the small-molecule CCR5 antagonists SCH-351125 and SCH-350581 inhibit human immunodeficiency virus type 1 entry. J. Virol. 2003, 77, 5201-5208.
-
(2003)
J. Virol.
, vol.77
, pp. 5201-5208
-
-
Tsamis, F.1
Gavrilov, S.2
Kajumo, F.3
Seibert, C.4
Kuhmann, S.5
Ketas, T.6
Trkola, A.7
Palani, A.8
Clader, J.W.9
Tagat, J.R.10
McCombie, S.11
Baroudy, B.12
Moore, J.P.13
Sakmar, T.P.14
Dragic, T.15
-
31
-
-
0035846070
-
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4-methyl-4-[3(S)-methyl-4-[1(S) -[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]-piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist
-
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.; Vantuno, N.; Baroudy, B. M.; Strizki, J. M. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4-methyl-4-[3(S)-methyl-4-[1(S) -[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]-piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist J. Med. Chem. 2001, 44, 3343-3346.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 3343-3346
-
-
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
Vantuno, N.11
Baroudy, B.M.12
Strizki, J.M.13
-
32
-
-
0035921055
-
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-Methyl piperazine as a key pharmacophore element
-
Tagat, J. R.; McCombie, S. W.; Steensma, R. W.; Lin, S.; Nazareno, D. V. ; Baroudy, B.; Vantuno, N.; Xu, S.; Liu, J. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-Methyl piperazine as a key pharmacophore element. Bioorg. Med. Chem. Lett. 2001, 11, 2143-2146.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2143-2146
-
-
Tagat, J.R.1
McCombie, S.W.2
Steensma, R.W.3
Lin, S.4
Nazareno, D.V.5
Baroudy, B.6
Vantuno, N.7
Xu, S.8
Liu, J.9
-
33
-
-
0037325553
-
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
-
McCombie, S. W.; Tagat, J. R.; Vice, S. F.; Lin, S. I.; Steensma, R.; Palani, A.; Neustadt, B. R.; Baroudy, B. M.; Strizki, J. M.; Endres, M. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides. Bioorg. Med. Chem. Lett. 2003, 13, 567-571.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 567-571
-
-
McCombie, S.W.1
Tagat, J.R.2
Vice, S.F.3
Lin, S.I.4
Steensma, R.5
Palani, A.6
Neustadt, B.R.7
Baroudy, B.M.8
Strizki, J.M.9
Endres, M.10
-
34
-
-
0034461768
-
Drug-like properties and the causes of poor solubility and poor permeability
-
Lipinski, C. A. Drug-like properties and the causes of poor solubility and poor permeability. J. Pharmacol. Toxicol. Methods 2000, 44, 235-249.
-
(2000)
J. Pharmacol. Toxicol. Methods
, vol.44
, pp. 235-249
-
-
Lipinski, C.A.1
-
35
-
-
0035289779
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
Lipinski, C. A.; Lombardo, F.; Dominy, B. W.; Feeney, P. J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Delivery Rev. 2001, 46, 3-26.
-
(2001)
Adv. Drug Delivery Rev.
, vol.46
, pp. 3-26
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
-
37
-
-
0037365448
-
Pharmacophore modeling as an efficient tool in the discovery of novel noncompetitive AMPA receptor antagonists
-
Barreca, M. L.; Gitto, R.; Quartarone, S.; De Luca, L.; De Sarro, G.; Chimirri, A. Pharmacophore modeling as an efficient tool in the discovery of novel noncompetitive AMPA receptor antagonists. J. Chem. Inf. Comput. Sci. 2003, 43, 651-655.
-
(2003)
J. Chem. Inf. Comput. Sci.
, vol.43
, pp. 651-655
-
-
Barreca, M.L.1
Gitto, R.2
Quartarone, S.3
De Luca, L.4
De Sarro, G.5
Chimirri, A.6
-
38
-
-
0001073278
-
The design of combinatorial libraries using properties and 3D pharmacophore fingerprints
-
Beno, B. R.; Mason, J. S. The design of combinatorial libraries using properties and 3D pharmacophore fingerprints. Drug Discovery Today 2001, 6, 251-258.
-
(2001)
Drug Discovery Today
, vol.6
, pp. 251-258
-
-
Beno, B.R.1
Mason, J.S.2
-
39
-
-
0033670977
-
A pharmacophore model for dopamine D4 receptor antagonists
-
Bostrom, J.; Gundertofte, K.; Liljeforsa, T. A pharmacophore model for dopamine D4 receptor antagonists. J. Comput.-Aided Mol. Des. 2000, 14, 769-786.
-
(2000)
J. Comput.-Aided Mol. Des.
, vol.14
, pp. 769-786
-
-
Bostrom, J.1
Gundertofte, K.2
Liljeforsa, T.3
-
40
-
-
0030341550
-
Pharmacophore development for antagonists at alpha 1 adrenergic receptor subtypes
-
Bremner, J. B.; Coban, B.; Griffith, R. Pharmacophore development for antagonists at alpha 1 adrenergic receptor subtypes. J. Comput.-Aided Mol. Des. 1996, 10, 545-557.
-
(1996)
J. Comput.-Aided Mol. Des.
, vol.10
, pp. 545-557
-
-
Bremner, J.B.1
Coban, B.2
Griffith, R.3
-
41
-
-
0034212669
-
Developing a dynamic pharmacophore model for HIV-1 integrase
-
Carlson, H. A.; Masukawa, K. M.; Rubins, K.; Bushman, F. D.; Jorgensen, W. L.; Lins, R. D.; Briggs, J. M.; McCammon, J. A. Developing a dynamic pharmacophore model for HIV-1 integrase. J. Med. Chem. 2000, 43, 2100-2114.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 2100-2114
-
-
Carlson, H.A.1
Masukawa, K.M.2
Rubins, K.3
Bushman, F.D.4
Jorgensen, W.L.5
Lins, R.D.6
Briggs, J.M.7
McCammon, J.A.8
-
42
-
-
0033193464
-
Automated pharmacophore identification for large chemical data sets
-
Chen, X.; Rusinko, A., III; Tropsha, A.; Young, S. S. Automated pharmacophore identification for large chemical data sets. J. Chem. Inf. Comput. Sci. 1999, 39, 887-896.
-
(1999)
J. Chem. Inf. Comput. Sci.
, vol.39
, pp. 887-896
-
-
Chen, X.1
Rusinko A. III2
Tropsha, A.3
Young, S.S.4
-
43
-
-
0037011895
-
Pharmacophore mapping of a series of 2,4-diamino-5-deazapteridine inhibitors of Mycobacterium avium complex dihydrofolate reductase
-
Debnath, A. K. Pharmacophore mapping of a series of 2,4-diamino-5-deazapteridine inhibitors of Mycobacterium avium complex dihydrofolate reductase. J. Med. Chem. 2002, 45, 41-53.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 41-53
-
-
Debnath, A.K.1
-
44
-
-
0034962557
-
Pharmacophore and three-dimensional quantitative structure activity relationship methods for modeling cytochrome p450 active sites
-
Ekins, S.; de Groot, M. J.; Jones, J. P. Pharmacophore and three-dimensional quantitative structure activity relationship methods for modeling cytochrome p450 active sites. Drug Metab. Dispos. 2001, 29, 936-944.
-
(2001)
Drug Metab. Dispos.
, vol.29
, pp. 936-944
-
-
Ekins, S.1
De Groot, M.J.2
Jones, J.P.3
-
45
-
-
0037389628
-
In vitro and pharmacophore insights into CYP3A enzymes
-
Ekins, S.; Stresser, D. M.; Andrew Williams, J. In vitro and pharmacophore insights into CYP3A enzymes. Trends Pharmacol. Sci. 2003, 24, 161-166.
-
(2003)
Trends Pharmacol. Sci.
, vol.24
, pp. 161-166
-
-
Ekins, S.1
Stresser, D.M.2
Andrew Williams, J.3
-
46
-
-
0037328212
-
Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors
-
Enyedy, I. J.; Sakamuri, S.; Zaman, W. A.; Johnson, K. M.; Wang, S. Pharmacophore-based discovery of substituted pyridines as novel dopamine transporter inhibitors. Bioorg. Med. Chem. Lett. 2003, 13, 513-517.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 513-517
-
-
Enyedy, I.J.1
Sakamuri, S.2
Zaman, W.A.3
Johnson, K.M.4
Wang, S.5
-
47
-
-
12944277104
-
A common pharmacophore for epothilone and taxanes: Molecular basis for drug resistance conferred by tubulin mutations in human cancer cells
-
Giannakakou, P.; Gussio, R.; Nogales, E.; Downing, K. H.; Zaharevitz, D. ; Bollbuck, B.; Poy, G.; Sackett, D.; Nicolaou, K. C.; Fojo, T. A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells. Proc. Natl. Acad. Sci. U.S.A. 2000, 97, 2904-2909.
-
(2000)
Proc. Natl. Acad. Sci. U.S.A.
, vol.97
, pp. 2904-2909
-
-
Giannakakou, P.1
Gussio, R.2
Nogales, E.3
Downing, K.H.4
Zaharevitz, D.5
Bollbuck, B.6
Poy, G.7
Sackett, D.8
Nicolaou, K.C.9
Fojo, T.10
-
48
-
-
0141882047
-
History and evolution of the pharmacophore concept in computer-aided drug design
-
Guner, O. F. History and evolution of the pharmacophore concept in computer-aided drug design. Curr. Top. Med. Chem. 2002, 2, 1321-1332.
-
(2002)
Curr. Top. Med. Chem.
, vol.2
, pp. 1321-1332
-
-
Guner, O.F.1
-
49
-
-
6444245560
-
Three-dimensional pharmacophore hypotheses of octopamine/tyramine agonists which inhibit [1-14C]acetate incorporation in Plodia interpunctella
-
Hirashima, A.; Eiraku, T.; Shigeta, Y.; Kuwano, E. Three-dimensional pharmacophore hypotheses of octopamine/tyramine agonists which inhibit [1-14C]acetate incorporation in Plodia interpunctella. Bioorg. Med. Chem. 2003, 11, 95-103.
-
(2003)
Bioorg. Med. Chem.
, vol.11
, pp. 95-103
-
-
Hirashima, A.1
Eiraku, T.2
Shigeta, Y.3
Kuwano, E.4
-
50
-
-
0037402105
-
Pharmacophore-based molecular docking to account for ligand flexibility
-
Joseph-McCarthy, D.; Thomas, B. E.; Belmarsh, M.; Moustakas, D.; Alvarez, J. C. Pharmacophore-based molecular docking to account for ligand flexibility. Proteins 2003, 51, 172-188.
-
(2003)
Proteins
, vol.51
, pp. 172-188
-
-
Joseph-McCarthy, D.1
Thomas, B.E.2
Belmarsh, M.3
Moustakas, D.4
Alvarez, J.C.5
-
51
-
-
1842864778
-
Identification of a stable chymase inhibitor using a pharmacophore-based database search
-
Koide, Y.; Tatsui, A.; Hasegawa, T.; Murakami, A.; Satoh, S.; Yamada, H. ; Kazayama, S.; Takahashi, A. Identification of a stable chymase inhibitor using a pharmacophore-based database search. Bioorg. Med. Chem. Lett. 2003, 13, 25-29.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 25-29
-
-
Koide, Y.1
Tatsui, A.2
Hasegawa, T.3
Murakami, A.4
Satoh, S.5
Yamada, H.6
Kazayama, S.7
Takahashi, A.8
-
52
-
-
0037468539
-
Non-peptide angiotensin II receptor antagonists: Chemical feature based pharmacophore identification
-
Krovat, E. M.; Langer, T. Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification. J. Med. Chem. 2003, 46, 716-726.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 716-726
-
-
Krovat, E.M.1
Langer, T.2
-
53
-
-
0034934377
-
Pharmacophore modeling and three-dimensional database searching for drug design using catalyst
-
Kurogi, Y.; Guner, O. F. Pharmacophore modeling and three-dimensional database searching for drug design using catalyst. Curr. Med. Chem. 2001, 8, 1035-1055.
-
(2001)
Curr. Med. Chem.
, vol.8
, pp. 1035-1055
-
-
Kurogi, Y.1
Guner, O.F.2
-
54
-
-
0038542930
-
Application of pharmacophore models for the design and synthesis of new anticonvulsant drugs
-
Malawska, B.; Scatturin, A. Application of pharmacophore models for the design and synthesis of new anticonvulsant drugs. Mini-Rev. Med. Chem. 2003, 3, 341-348.
-
(2003)
Mini-Rev. Med. Chem.
, vol.3
, pp. 341-348
-
-
Malawska, B.1
Scatturin, A.2
-
55
-
-
0033606951
-
Lead generation using pharmacophore mapping and three-dimensional database searching: Application to muscarinic M(3) receptor antagonists
-
Marriott, D. P.; Dougall, I. G.; Meghani, P.; Liu, Y. J.; Flower, D. R. Lead generation using pharmacophore mapping and three-dimensional database searching: application to muscarinic M(3) receptor antagonists. J. Med. Chem. 1999, 42, 3210-3216.
-
(1999)
J. Med. Chem.
, vol.42
, pp. 3210-3216
-
-
Marriott, D.P.1
Dougall, I.G.2
Meghani, P.3
Liu, Y.J.4
Flower, D.R.5
-
56
-
-
0036706746
-
A comparison of the pharmacophore identification programs: Catalyst, DISCO and GASP
-
Patel, Y.; Gillet, V. J.; Bravi, G.; Leach, A. R. A comparison of the pharmacophore identification programs: Catalyst, DISCO and GASP. J. Comput.-Aided Mol. Des. 2002, 16, 653-681.
-
(2002)
J. Comput.-Aided Mol. Des.
, vol.16
, pp. 653-681
-
-
Patel, Y.1
Gillet, V.J.2
Bravi, G.3
Leach, A.R.4
-
57
-
-
0037374498
-
The price of innovation: New estimates of drug development costs
-
DiMasi, J. A.; Hansen, R. W.; Grabowski, H. G. The price of innovation: new estimates of drug development costs. J. Health Econ. 2003, 22, 151-185.
-
(2003)
J. Health Econ.
, vol.22
, pp. 151-185
-
-
DiMasi, J.A.1
Hansen, R.W.2
Grabowski, H.G.3
-
58
-
-
0037325553
-
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
-
McCombie, S. W.; Tagat, J. R.; Vice, S. F.; Lin, S. I.; Steensma, R.; Palani, A.; Neustadt, B. R.; Baroudy, B. M.; Strizki, J. M.; Endres, M.; Cox, K.; Dan, N.; Chou, C. C. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides. Bioorg. Med. Chem. Lett. 2003, 13, 567-571.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 567-571
-
-
McCombie, S.W.1
Tagat, J.R.2
Vice, S.F.3
Lin, S.I.4
Steensma, R.5
Palani, A.6
Neustadt, B.R.7
Baroudy, B.M.8
Strizki, J.M.9
Endres, M.10
Cox, K.11
Dan, N.12
Chou, C.C.13
-
59
-
-
0037294907
-
Oximinopiperidino-piperidine-based CCR5 antagonists. Part 2: Synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides
-
Palani, A.; Shapiro, S.; Clader, J. W.; Greenlee, W. J.; Vice, S.; McCombie, S.; Cox, K.; Strizki, J.; Baroudy, B. M. Oximinopiperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides. Bioorg. Med. Chem. Lett. 2003, 13, 709-712.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 709-712
-
-
Palani, A.1
Shapiro, S.2
Clader, J.W.3
Greenlee, W.J.4
Vice, S.5
McCombie, S.6
Cox, K.7
Strizki, J.8
Baroudy, B.M.9
-
60
-
-
0001383234
-
HypoGen: An automated system for generating 3D predictive pharmacophore models
-
Guner, O. F., Ed.; International University Line: La Jolla, CA
-
Li, H.; Sutter, J.; Hoffman, R. HypoGen: An automated system for generating 3D predictive pharmacophore models. In Pharmacophore Perception, Development, and Use in Drug Design; Guner, O. F., Ed.; International University Line: La Jolla, CA, 1999; pp 173-189.
-
(1999)
Pharmacophore Perception, Development, and Use in Drug Design
, pp. 173-189
-
-
Li, H.1
Sutter, J.2
Hoffman, R.3
-
61
-
-
84986512474
-
CHARMM: A program for macromolecular energy, minimization, and dynamics calculations
-
Brooks, B. R.; Bruccoleri, R. E.; Olafson, B. D.; States, D. J.; Swaminathan, S.; Karplus, M. CHARMM: A Program for Macromolecular Energy, Minimization, and Dynamics Calculations. J. Comput. Chem. 1983, 4, 187-217.
-
(1983)
J. Comput. Chem.
, vol.4
, pp. 187-217
-
-
Brooks, B.R.1
Bruccoleri, R.E.2
Olafson, B.D.3
States, D.J.4
Swaminathan, S.5
Karplus, M.6
-
62
-
-
84986522856
-
Poling: Promoting conformational variation
-
Smellie, A. Poling: Promoting Conformational Variation. J. Comput. Chem. 1995, 16, 171-187.
-
(1995)
J. Comput. Chem.
, vol.16
, pp. 171-187
-
-
Smellie, A.1
-
63
-
-
0029277503
-
Analysis of conformational coverage. 1. Validation and estimation of coverage
-
Smellie, A.; Kahn, S. D.; Teig, S. L. Analysis of Conformational Coverage. 1. Validation and Estimation of Coverage. J. Chem. Inf. Comput. Sci. 1995, 35, 285-294.
-
(1995)
J. Chem. Inf. Comput. Sci.
, vol.35
, pp. 285-294
-
-
Smellie, A.1
Kahn, S.D.2
Teig, S.L.3
-
64
-
-
0029276206
-
Analysis of conformational space. 2. Application of conformational models
-
Smellie, A.; Kahn, S. D.; Teig, S. L. Analysis of Conformational Space. 2. Application of Conformational Models J. Chem. Inf. Comput. Sci. 1995, 16, 295-304.
-
(1995)
J. Chem. Inf. Comput. Sci.
, vol.16
, pp. 295-304
-
-
Smellie, A.1
Kahn, S.D.2
Teig, S.L.3
-
65
-
-
0004549354
-
Effect of variable weight and tolerances on predictive model generation
-
Guner, O. F., Ed.; International University Line: La Jolla, CA
-
Sutter, J.; Güner, O. F.; Hoffman, R.; Li, H.; Waldman, M. Effect of Variable Weight and Tolerances on Predictive Model Generation. In Pharmacophore Perception, Development, and Use in Drug Design; Guner, O. F., Ed.; International University Line: La Jolla, CA, 1999; pp 501-511.
-
(1999)
Pharmacophore Perception, Development, and Use in Drug Design
, pp. 501-511
-
-
Sutter, J.1
Güner, O.F.2
Hoffman, R.3
Li, H.4
Waldman, M.5
-
66
-
-
0141916591
-
Inhibitors of calling behavior of Plodia interpunctella
-
Hirashima, A.; Shigeta, Y.; Eiraku, T.; Kuwano, E. Inhibitors of Calling Behavior of Plodia interpunctella. J. Insect Sci. 2003, 3, 4.
-
(2003)
J. Insect Sci.
, vol.3
, pp. 4
-
-
Hirashima, A.1
Shigeta, Y.2
Eiraku, T.3
Kuwano, E.4
-
67
-
-
0036888354
-
Mining the chemical abstracts database with pharmacophore-based queries
-
Bremner, J. B.; Castle, K.; Griffith, R.; Keller, P. A.; Ridley, D. D. Mining the Chemical Abstracts database with pharmacophore-based queries. J. Mol. Graphics Modell. 2002, 21, 185-194.
-
(2002)
J. Mol. Graphics Modell.
, vol.21
, pp. 185-194
-
-
Bremner, J.B.1
Castle, K.2
Griffith, R.3
Keller, P.A.4
Ridley, D.D.5
-
68
-
-
0030253210
-
Active-site-directed 3D database searching: Pharmacophore extraction and validation of hits
-
Clark, D. E.; Westhead, D. R.; Sykes, R. A.; Murray, C. W. Active-site-directed 3D database searching: pharmacophore extraction and validation of hits. J. Comput.-Aided Mol. Des. 1996, 10, 397-416.
-
(1996)
J. Comput.-Aided Mol. Des.
, vol.10
, pp. 397-416
-
-
Clark, D.E.1
Westhead, D.R.2
Sykes, R.A.3
Murray, C.W.4
-
69
-
-
0030891601
-
HIV-1 integrase pharmacophore: Discovery of inhibitors through three-dimensional database searching
-
Nicklaus, M. C.; Neamati, N.; Hong, H.; Mazumder, A.; Sunder, S.; Chen, J.; Milne, G. W.; Pommier, Y. HIV-1 integrase pharmacophore: discovery of inhibitors through three-dimensional database searching. J. Med. Chem. 1997, 40, 920-929.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 920-929
-
-
Nicklaus, M.C.1
Neamati, N.2
Hong, H.3
Mazumder, A.4
Sunder, S.5
Chen, J.6
Milne, G.W.7
Pommier, Y.8
-
70
-
-
0005123846
-
Automated chemical hypothesis generation and database searching with catalyst
-
Müller, K., Ed.; ESCOM Science Publishers B.V.: Leiden, The Netherlands
-
Sprague, P. W. Automated chemical hypothesis generation and database searching with Catalyst. In Perspectives in Drug Discovery and Design; Müller, K., Ed.; ESCOM Science Publishers B.V.: Leiden, The Netherlands, 1995; pp 1-21.
-
(1995)
Perspectives in Drug Discovery and Design
, pp. 1-21
-
-
Sprague, P.W.1
-
71
-
-
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.; Siciliano, S.; Malkowitz, L.; Schleif, W. A.; Hazuda, D.; Miller, M.; Kessler, J.; Danzeisen, R.; Holmes, K.; Lineberger, J.; Carella, A.; Carver, G.; Emini, E. 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. 2001, 11, 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
Siciliano, S.11
Malkowitz, L.12
Schleif, W.A.13
Hazuda, D.14
Miller, M.15
Kessler, J.16
Danzeisen, R.17
Holmes, K.18
Lineberger, J.19
Carella, A.20
Carver, G.21
Emini, E.22
more..
-
72
-
-
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.; Malkowitz, L.; Siciliano, S.; Gould, S. L.; DeMartino, J. A.; Springer, M. S. 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. 2001, 11, 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
Malkowitz, L.5
Siciliano, S.6
Gould, S.L.7
DeMartino, J.A.8
Springer, M.S.9
-
73
-
-
18644374488
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: Polar functionality and its effect on anti-HIV-1 activity
-
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. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity. Bioorg. Med. Chem. Lett. 2002, 12, 2997-3000.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2997-3000
-
-
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
-
74
-
-
18644372005
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: Synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV
-
Lynch, C. L.; Hale, J. J.; Budhu, R. J.; Gentry, A. L.; Mills, S. G.; Chapman, K. T.; MacCoss, M.; Malkowitz, L.; Springer, M. S.; Gould, S. L. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: Synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV. Bioorg. Med. Chem. Lett. 2002, 12, 3001-3004.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 3001-3004
-
-
Lynch, C.L.1
Hale, J.J.2
Budhu, R.J.3
Gentry, A.L.4
Mills, S.G.5
Chapman, K.T.6
MacCoss, M.7
Malkowitz, L.8
Springer, M.S.9
Gould, S.L.10
-
75
-
-
18744416543
-
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: Modifications of the arylpropylpiperidine side chains
-
Lynch, C. L.; Willoughby, C. A.; Hale, J. J.; Holson, E. J.; Budhu, R. J.; Gentry, A. L.; Rosauer, K. G.; Caldwell, C. G.; Chen, P.; Mills, S. G. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains. Bioorg. Med. Chem. Lett. 2003, 13, 119-123.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 119-123
-
-
Lynch, C.L.1
Willoughby, C.A.2
Hale, J.J.3
Holson, E.J.4
Budhu, R.J.5
Gentry, A.L.6
Rosauer, K.G.7
Caldwell, C.G.8
Chen, P.9
Mills, S.G.10
-
76
-
-
18244396143
-
CCR5 antagonists: Bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines
-
Lynch, C. L.; Gentry, A. L.; Hale, J. J.; Mills, S. G.; MacCoss, M.; Malkowitz, L.; Springer, M. S.; Gould, S. L.; DeMartino, J. A.; Siciliano, S. J. CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines. Bioorg. Med. Chem. Lett. 2002, 12, 677-679.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 677-679
-
-
Lynch, C.L.1
Gentry, A.L.2
Hale, J.J.3
Mills, S.G.4
MacCoss, M.5
Malkowitz, L.6
Springer, M.S.7
Gould, S.L.8
DeMartino, J.A.9
Siciliano, S.J.10
-
77
-
-
12244267994
-
Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: A molecular modeling-guided mutagenesis study of the binding pocket
-
Castonguay, L. A.; Weng, Y.; Adolfsen, W.; Di Salvo, J.; Kilburn, R.; Caldwell, C. G.; Daugherty, B. L.; Finke, P. E.; Hale, J. J.; Lynch, C. L.; Mills, S. G.; MacCoss, M.; Springer, M. S.; DeMartino, J. A. Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket. Biochemistry 2003, 42, 1544-1550.
-
(2003)
Biochemistry
, vol.42
, pp. 1544-1550
-
-
Castonguay, L.A.1
Weng, Y.2
Adolfsen, W.3
Di Salvo, J.4
Kilburn, R.5
Caldwell, C.G.6
Daugherty, B.L.7
Finke, P.E.8
Hale, J.J.9
Lynch, C.L.10
Mills, S.G.11
MacCoss, M.12
Springer, M.S.13
DeMartino, J.A.14
-
78
-
-
0035931442
-
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationships for 1-amino-2-phenyl-4-(piperidin-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.; DeMartino, J. A.; Siciliano, S. J.; Carella, A.; Carver, G.; Holmes, K.; Danzeisen, R.; Hazuda, D.; Kessler, J.; Lineberger, J.; Miller, M.; Schleif, W. A.; Emini, E. A. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: discovery and initial structure-activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. 2001, 11, 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
DeMartino, J.A.11
Siciliano, S.J.12
Carella, A.13
Carver, G.14
Holmes, K.15
Danzeisen, R.16
Hazuda, D.17
Kessler, J.18
Lineberger, J.19
Miller, M.20
Schleif, W.A.21
Emini, E.A.22
more..
-
79
-
-
17944365465
-
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl) -N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes
-
Finke, P. E.; Oates, B.; Mills, S. G.; MacCoss, M.; Malkowitz, L.; Springer, M. S.; Gould, S. L.; DeMartino, J. A.; Carella, A.; Carver, G.; Holmes, K.; Danzeisen, R.; Hazuda, D.; Kessler, J.; Lineberger, J.; Miller, M.; Schleif, W. A.; Emini, E. A. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl) -N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. 2001, 11, 2475-2479.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2475-2479
-
-
Finke, P.E.1
Oates, B.2
Mills, S.G.3
MacCoss, M.4
Malkowitz, L.5
Springer, M.S.6
Gould, S.L.7
DeMartino, J.A.8
Carella, A.9
Carver, G.10
Holmes, K.11
Danzeisen, R.12
Hazuda, D.13
Kessler, J.14
Lineberger, J.15
Miller, M.16
Schleif, W.A.17
Emini, E.A.18
-
80
-
-
17944379325
-
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: A proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-[4-(substituted) piperidin-1-yl]butanes
-
Finke, P. E.; Meurer, L. C.; Oates, B.; Shah, S. K.; Loebach, J. L.; Mills, S. G.; MacCoss, M.; Castonguay, L.; Malkowitz, L.; Springer, M. S.; Gould, S. L.; DeMartino, J. A. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: a proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-[4-(substituted) piperidin-1-yl]butanes. Bioorg. Med. Chem. Lett. 2001, 11, 2469-2473.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 2469-2473
-
-
Finke, P.E.1
Meurer, L.C.2
Oates, B.3
Shah, S.K.4
Loebach, J.L.5
Mills, S.G.6
MacCoss, M.7
Castonguay, L.8
Malkowitz, L.9
Springer, M.S.10
Gould, S.L.11
DeMartino, J.A.12
-
81
-
-
0035931392
-
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationships 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.; Siciliano, S. J.; Carella, A.; Carver, G.; Holmes, K.; Danzeisen, R.; Hazuda, D.; Kessler, J.; Lineberger, J.; Miller, M.; Schleif, W. A.; Emini, E. A. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes. Bioorg. Med. Chem. Lett. 2001, 11, 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
Siciliano, S.J.11
Carella, A.12
Carver, G.13
Holmes, K.14
Danzeisen, R.15
Hazuda, D.16
Kessler, J.17
Lineberger, J.18
Miller, M.19
Schleif, W.A.20
Emini, E.A.21
more..
-
82
-
-
0035904879
-
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection
-
Kim, D.; Wang, L.; Caldwell, C. G.; Chen, P.; Finke, P. E.; Oates, B.; MacCoss, M.; Mills, S. G.; Malkowitz, L.; Gould, S. L.; DeMartino, J. A.; Springer, M. S.; Hazuda, D.; Miller, M.; Kessler, J.; Danzeisen, R.; Carver, G. ; Carella, A.; Holmes, K.; Lineberger, J.; Schleif, W. A.; Emini, E. A. Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection. Bioorg. Med. Chem. Lett. 2001, 11, 3103-3106.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 3103-3106
-
-
Kim, D.1
Wang, L.2
Caldwell, C.G.3
Chen, P.4
Finke, P.E.5
Oates, B.6
MacCoss, M.7
Mills, S.G.8
Malkowitz, L.9
Gould, S.L.10
DeMartino, J.A.11
Springer, M.S.12
Hazuda, D.13
Miller, M.14
Kessler, J.15
Danzeisen, R.16
Carver, G.17
Carella, A.18
Holmes, K.19
Lineberger, J.20
Schleif, W.A.21
Emini, E.A.22
more..
-
83
-
-
0035904880
-
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection
-
Kim, D.; Wang, L.; Caldwell, C. G.; Chen, P.; Finke, P. E.; Oates, B.; MacCoss, M.; Mills, S. G.; Malkowitz, L.; Gould, S. L.; DeMartino, J. A.; Springer, M. S.; Hazuda, D.; Miller, M.; Kessler, J.; Danzeisen, R.; Carver, G. ; Carella, A.; Holmes, K.; Lineberger, J.; Schleif, W. A.; Emini, E. A. Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection. Bioorg. Med. Chem. Lett. 2001, 11, 3099-3102.
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 3099-3102
-
-
Kim, D.1
Wang, L.2
Caldwell, C.G.3
Chen, P.4
Finke, P.E.5
Oates, B.6
MacCoss, M.7
Mills, S.G.8
Malkowitz, L.9
Gould, S.L.10
DeMartino, J.A.11
Springer, M.S.12
Hazuda, D.13
Miller, M.14
Kessler, J.15
Danzeisen, R.16
Carver, G.17
Carella, A.18
Holmes, K.19
Lineberger, J.20
Schleif, W.A.21
Emini, E.A.22
more..
-
84
-
-
0141882046
-
-
Piperidines as CCR5 Modulators. Patent WO 00/39125, 2000
-
Armour, D. R.; Price, D. A.; Stammen, B. L. C.; Wood, A.; Perros, M.; Edwards, M. P. Piperidines as CCR5 Modulators. Patent WO 00/39125, 2000.
-
-
-
Armour, D.R.1
Price, D.A.2
Stammen, B.L.C.3
Wood, A.4
Perros, M.5
Edwards, M.P.6
-
85
-
-
0141882045
-
-
Aminoazacycloalkanase as CCR5 modulators. Patent EP-1013276, 2000
-
Armour, D. R.; Price, D. A.; Stammen, B. L. C.; Wood, A.; Perros, M.; Edwards, M. P. Aminoazacycloalkanase as CCR5 modulators. Patent EP-1013276, 2000.
-
-
-
Armour, D.R.1
Price, D.A.2
Stammen, B.L.C.3
Wood, A.4
Perros, M.5
Edwards, M.P.6
-
86
-
-
0141950965
-
-
Propenamides as CCR5 Modulators. Patent WO 00/06153, 2000
-
Bondinell, W. E. Propenamides as CCR5 Modulators. Patent WO 00/06153, 2000.
-
-
-
Bondinell, W.E.1
-
87
-
-
0141916592
-
-
Substituted Anilide Compounds and Methods. Patent WO 00/06146, 2000
-
Ku, T. W.; Bondinell, W. E.; Neeb, M. J. Substituted Anilide Compounds and Methods. Patent WO 00/06146, 2000.
-
-
-
Ku, T.W.1
Bondinell, W.E.2
Neeb, M.J.3
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