-
2
-
-
77956803052
-
Recent advances in the development of HIV reverse transcriptase inhibitors
-
Romero, D. L. Recent Advances in the Development of HIV Reverse Transcriptase Inhibitors. Annu. Rep. Med. Chem. 1994, 29, 123-132.
-
(1994)
Annu. Rep. Med. Chem.
, vol.29
, pp. 123-132
-
-
Romero, D.L.1
-
3
-
-
0029969537
-
Antiretroviral drug resistance: Mechanisms, pathogenesis, clinical significance
-
Richman, D. D. Antiretroviral Drug Resistance: Mechanisms, Pathogenesis, Clinical Significance. Adv. Exp. Med. Biol. 1996, 394, 383-395.
-
(1996)
Adv. Exp. Med. Biol.
, vol.394
, pp. 383-395
-
-
Richman, D.D.1
-
4
-
-
0029877185
-
Efficacy of combination antiretroviral therapy
-
Collier, A. C. Efficacy of Combination Antiretroviral Therapy. Adv. Exp. Med. Biol. 1996, 394, 383-395.
-
(1996)
Adv. Exp. Med. Biol.
, vol.394
, pp. 383-395
-
-
Collier, A.C.1
-
5
-
-
0029729543
-
Combination therapy in the management of HIV infection
-
Vella, S.; France Pirillo, M. Combination Therapy in the Management of HIV Infection. Methods Find. Exp. Clin. Pharm. 1996, 18 (Suppl. C), 23-26.
-
(1996)
Methods Find. Exp. Clin. Pharm.
, vol.18
, Issue.SUPPL. C
, pp. 23-26
-
-
Vella, S.1
France Pirillo, M.2
-
6
-
-
0028207314
-
Delavirdine mesylate
-
(a) Romero, D. L. Delavirdine Mesylate. Drugs Future 1994, 19 (1), 9-12.
-
(1994)
Drugs Future
, vol.19
, Issue.1
, pp. 9-12
-
-
Romero, D.L.1
-
7
-
-
0029038353
-
BHAPs
-
(b) Aristoff, P. A. BHAPs. DN&P 1995, 8 (3), 151-155.
-
(1995)
DN&P
, vol.8
, Issue.3
, pp. 151-155
-
-
Aristoff, P.A.1
-
8
-
-
0025679303
-
Inhibition of HIV-1 replication by a non-nucleoside reverse transcriptase inhibitor
-
Merluzzi, V. J.; Hargrave, K. D.; Labadia, M.; Grozinger, K.; Skoog, M.; Wu, J. C.; Shih, C.-K.; Eckner, K.; Hattox, S.; Adams, J.; Rosenthal, A. S.; Faanes, R.; Eckner, R. J.; Koup, R. A.; Sullivan, J. L. Inhibition of HIV-1 Replication by a Non-Nucleoside Reverse Transcriptase Inhibitor. Science 1990, 250, 1411-1413.
-
(1990)
Science
, vol.250
, pp. 1411-1413
-
-
Merluzzi, V.J.1
Hargrave, K.D.2
Labadia, M.3
Grozinger, K.4
Skoog, M.5
Wu, J.C.6
Shih, C.-K.7
Eckner, K.8
Hattox, S.9
Adams, J.10
Rosenthal, A.S.11
Faanes, R.12
Eckner, R.J.13
Koup, R.A.14
Sullivan, J.L.15
-
9
-
-
0025740266
-
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo-and dipyridodiazepinones
-
Hargrave, K. D.; Proudfoot, J. R.; Grozinger, K. G.; Kapadia, S. R.; Patel, U. R.; Fuchs, V. U.; Mauldin, S. C.; Vitous, J.; Behnke, M. L.; Klunder, J. M.; Pal, K.; Skiles, J. W.; McNeil, D. W.; Rose, J. M.; Chow, G. C.; Skoog, M. T.; Wu, J. C.; Schmidt, G.; Engel, W.; Eberlein, W. G.; Saboe, T. D.; Campbell, S. J.; Rosenthal, A. S.; Adams, J. Novel Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 1. Tricyclic Pyridobenzo-and Dipyridodiazepinones. J. Med. Chem. 1981, 34, 2231-2241.
-
(1981)
J. Med. Chem.
, vol.34
, pp. 2231-2241
-
-
Hargrave, K.D.1
Proudfoot, J.R.2
Grozinger, K.G.3
Kapadia, S.R.4
Patel, U.R.5
Fuchs, V.U.6
Mauldin, S.C.7
Vitous, J.8
Behnke, M.L.9
Klunder, J.M.10
Pal, K.11
Skiles, J.W.12
McNeil, D.W.13
Rose, J.M.14
Chow, G.C.15
Skoog, M.T.16
Wu, J.C.17
Schmidt, G.18
Engel, W.19
Eberlein, W.G.20
Saboe, T.D.21
Campbell, S.J.22
Rosenthal, A.S.23
Adams, J.24
more..
-
10
-
-
0031944616
-
Efavirenz
-
(a) Graul, A.; Rabasseda, X.; Castaner, J. Efavirenz. Drugs Future 1998, 23 (2), 133-141.
-
(1998)
Drugs Future
, vol.23
, Issue.2
, pp. 133-141
-
-
Graul, A.1
Rabasseda, X.2
Castaner, J.3
-
11
-
-
0028785708
-
L-743,726 (DMP-266): A novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase
-
(b) Young, S. D.; Britcher, S. F.; Tran, L. O.; Payne, L. S.; Lumma, W. C.; Lyle, T. A.; Huff, J. R.; Anderson, P. S.; Olsen, D. B.; Carroll, S. S.; Pettibone, D. J.; O'Brien, J. A.; Ball, R. G.; Balani, S. K.; Lin, J. H.; Chen, I-W.; Schleif, W. A.; Sardana, V. V.; Long, W. J.; Byrnes, V. W.; Emini, E. A. L-743,726 (DMP-266): a Novel, Highly Potent Nonnucleoside Inhibitor of the Human Immunodeficiency Virus Type 1 Reverse Transcriptase. Antimicrob. Agents Chemother. 1995, 39 (12), 2602-2605.
-
(1995)
Antimicrob. Agents Chemother
, vol.39
, Issue.12
, pp. 2602-2605
-
-
Young, S.D.1
Britcher, S.F.2
Tran, L.O.3
Payne, L.S.4
Lumma, W.C.5
Lyle, T.A.6
Huff, J.R.7
Anderson, P.S.8
Olsen, D.B.9
Carroll, S.S.10
Pettibone, D.J.11
O'Brien, J.A.12
Ball, R.G.13
Balani, S.K.14
Lin, J.H.15
Chen, I.-W.16
Schleif, W.A.17
Sardana, V.V.18
Long, W.J.19
Byrnes, V.W.20
Emini, E.A.21
more..
-
12
-
-
0028229645
-
How to overcome resistance of HIV-1 to HIV-1 specific reverse transcriptase inhibitors
-
(a) de Clercq, E. How to overcome resistance of HIV-1 to HIV-1 specific reverse transcriptase inhibitors. AIDS 1994, 8 (7), 1020-1021.
-
(1994)
AIDS
, vol.8
, Issue.7
, pp. 1020-1021
-
-
De Clercq, E.1
-
13
-
-
0029877789
-
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of human immunodeficiency virus type 1 (HIV-1) infections: Strategies to overcome drug resistance development
-
(b) de Clercq, E. Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs) for the Treatment of Human Immunodeficiency Virus Type 1 (HIV-1) Infections: Strategies to Overcome Drug Resistance Development. Med. Res. Rev. 1996, 16, 125.
-
(1996)
Med. Res. Rev.
, vol.16
, pp. 125
-
-
De Clercq, E.1
-
14
-
-
0027231438
-
A mutation in reverse transcriptase of bis(heteroaryl)piperazine resistant human immundeficiency virus type 1 that confers increased sensitivity to other nonnucleoside inhibitors
-
Dueweke, T. J.; Pushkarskaya, T.; Poppe, S. M.; Swaney, S. M.; Zhao, J. Q.; Chen, I. S. Y.; Stevenson, M.; Tarpley, W. G. A mutation in reverse transcriptase of bis(heteroaryl)piperazine resistant human immundeficiency virus type 1 that confers increased sensitivity to other nonnucleoside inhibitors. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 4813-4717.
-
(1993)
Proc. Natl. Acad. Sci. U.S.A.
, vol.90
, pp. 4813-14717
-
-
Dueweke, T.J.1
Pushkarskaya, T.2
Poppe, S.M.3
Swaney, S.M.4
Zhao, J.Q.5
Chen, I.S.Y.6
Stevenson, M.7
Tarpley, W.G.8
-
15
-
-
9544229686
-
Targeting delavirdine/atevirdine resistant HIV-1: Identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors
-
Romero, D. L.; Olmsted, R. A.; Poel, T. J.; Morge, R. A.; Biles, C.; Keiser, B. J.; Kopta, L. A.; Friis, J. M.; Hosley, J. D.; Stefanski, K. J.; Wishka, D. G.; Evans, D. B.; Morris, J., Stehle, R. G.; Sharma, S. K.; Yagi, Y.; Voorman, R. L.; Adams, W. J.; Tarpley, W. G.; Thomas, R. C. Targeting Delavirdine/Atevirdine Resistant HIV-1: Identification of (Alkylamino)piperidine-Containing Bis(heteroaryl)piperazines as Broad Spectrum HIV-1 Reverse Transcriptase Inhibitors. J. Med. Chem. 1996, 39, 3769-3789.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 3769-3789
-
-
Romero, D.L.1
Olmsted, R.A.2
Poel, T.J.3
Morge, R.A.4
Biles, C.5
Keiser, B.J.6
Kopta, L.A.7
Friis, J.M.8
Hosley, J.D.9
Stefanski, K.J.10
Wishka, D.G.11
Evans, D.B.12
Morris, J.13
Stehle, R.G.14
Sharma, S.K.15
Yagi, Y.16
Voorman, R.L.17
Adams, W.J.18
Tarpley, W.G.19
Thomas, R.C.20
more..
-
16
-
-
0032560237
-
(-)-6-chloro-2-[(1-furo[2,3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor
-
Wishka, D. G.; Graber, D. R.; Kopta, L. A.; Olmsted, R. A.; Friis, J. M.; Hosley, J. D.; Adams, W. J.; Seest, E. P.; Castle, T. M.; Dolak, L. A.; Keiser, B. J.; Yagi, Y.; Azhwarsamy, J.; Schlachter, S. T.; Murphy M. J.; Cleek, G. J.; Nugent, R. A.; Poppe, S. M.; Swaney, S. M.; Han, F.; Watt, W.; White, W. L.; Poel, T.-J.; Thomas, R. C.; Voorman, R. L.; Stefanski, K. J.; Stehle, R. G.; Tarpley, W. G.; Morris, J. (-)-6-Chloro-2-[(1-furo[2,3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a New Broad Spectrum HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor. J. Med. Chem. 1998, 41, 1357-1360.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 1357-1360
-
-
Wishka, D.G.1
Graber, D.R.2
Kopta, L.A.3
Olmsted, R.A.4
Friis, J.M.5
Hosley, J.D.6
Adams, W.J.7
Seest, E.P.8
Castle, T.M.9
Dolak, L.A.10
Keiser, B.J.11
Yagi, Y.12
Azhwarsamy, J.13
Schlachter, S.T.14
Murphy, M.J.15
Cleek, G.J.16
Nugent, R.A.17
Poppe, S.M.18
Swaney, S.M.19
Han, F.20
Watt, W.21
White, W.L.22
Poel, T.-J.23
Thomas, R.C.24
Voorman, R.L.25
Stefanski, K.J.26
Stehle, R.G.27
Tarpley, W.G.28
Morris, J.29
more..
-
17
-
-
14444278270
-
Pyrimidine thioethers: A novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP resistant HIV
-
Nugent, R. A.; Schlachter, S. T.; Murphy, M. J.; Cleek, G. J.; Poel, T. J.; Wishka, D. G.; Graber, D. R.; Yagi, Y.; Keiser, B. J.; Olmsted, R. A.; Kopta, L. A.; Swaney, S. M.; Poppe, S. M.; Morris, J.; Tarpley, W. G.; Thomas, R. C. Pyrimidine Thioethers: A Novel Class of HIV-1 Reverse Transcriptase Inhibitors with Activity Against BHAP Resistant HIV. J. Med. Chem. 1998, 41, 3793-3803.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 3793-3803
-
-
Nugent, R.A.1
Schlachter, S.T.2
Murphy, M.J.3
Cleek, G.J.4
Poel, T.J.5
Wishka, D.G.6
Graber, D.R.7
Yagi, Y.8
Keiser, B.J.9
Olmsted, R.A.10
Kopta, L.A.11
Swaney, S.M.12
Poppe, S.M.13
Morris, J.14
Tarpley, W.G.15
Thomas, R.C.16
-
18
-
-
5544231319
-
Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: Structure-activity relationships and increased metabolic stability of novel substituted pyridine analogues
-
Genin, M. J.; Poel, T. J.; Yagi, Y.; Biles, C.; Althaus, I.; Keiser, B. J.; Kopta, L. A.; Friis, J. M.; Reusser, F.; Adams, W. J.; Olmsted, R. A.; Voorman, R. L.; Thomas, R. C.; Romero, D. L. Synthesis and Bioactivity of Novel Bis(heteroaryl)piperazine (BHAP) Reverse Transcriptase Inhibitors: Structure-Activity Relationships and Increased Metabolic Stability of Novel Substituted Pyridine Analogues. J. Med. Chem. 1996, 39, 5267-5275.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 5267-5275
-
-
Genin, M.J.1
Poel, T.J.2
Yagi, Y.3
Biles, C.4
Althaus, I.5
Keiser, B.J.6
Kopta, L.A.7
Friis, J.M.8
Reusser, F.9
Adams, W.J.10
Olmsted, R.A.11
Voorman, R.L.12
Thomas, R.C.13
Romero, D.L.14
-
19
-
-
0027304832
-
Improved syntheses of 2-bromonicotinaldehyde and acid
-
Melnyk, P.; Gasche, J.; Thai, C. Improved syntheses of 2-bromonicotinaldehyde and acid. Synth. Commun. 1993, 23 (19), 2727-2730.
-
(1993)
Synth. Commun.
, vol.23
, Issue.19
, pp. 2727-2730
-
-
Melnyk, P.1
Gasche, J.2
Thai, C.3
-
20
-
-
0344979645
-
-
note
-
Metabolites of the alkylpyridine-substituted AAP-BHAPs tend to be hydroxylated in the side chain or on the pyridine ring. There was also some N-dealkylation of the 4-(alkylamino)-piperidine nitrogen. In general, compounds with these modifications have not shown good inhibition of HIV RT.
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