-
1
-
-
0026579208
-
The HIV-1 Protease as a Therapeutic Target for AIDS
-
For recent reviews, see: (a) Debouck, C. The HIV-1 Protease as a Therapeutic Target for AIDS. AIDS Res. Human Retroviruses 1992, 8, 153-164.
-
(1992)
AIDS Res. Human Retroviruses
, vol.8
, pp. 153-164
-
-
Debouck, C.1
-
3
-
-
0005241362
-
Active Human Immunodeficiency Virus Protease is Required for Viral Infectivity
-
(a) Kohl, N. E.; Emini, E. A.; Schleif, W. A.; Davis, L. J.; Heimbach, J. C.; Dixon, R. A. F.; Scolnick, E. M.; Sigal, I. S. Active Human Immunodeficiency Virus Protease is Required for Viral Infectivity. Proc. Natl. Acad. Sci. U.S.A. 1988, 85, 4686-4690.
-
(1988)
Proc. Natl. Acad. Sci. U.S.A.
, vol.85
, pp. 4686-4690
-
-
Kohl, N.E.1
Emini, E.A.2
Schleif, W.A.3
Davis, L.J.4
Heimbach, J.C.5
Dixon, R.A.F.6
Scolnick, E.M.7
Sigal, I.S.8
-
4
-
-
0024334170
-
Role of Human Immunodeficiency Virus Type 1-Specific Protease in Core Protein Maturation and Viral Infectivity
-
(b) Peng, C.; Ho, B. K.; Chang, T. W.; Chang, N. T. Role of Human Immunodeficiency Virus Type 1-Specific Protease in Core Protein Maturation and Viral Infectivity. J. Virol. 1989, 63, 2550-2556.
-
(1989)
J. Virol.
, vol.63
, pp. 2550-2556
-
-
Peng, C.1
Ho, B.K.2
Chang, T.W.3
Chang, N.T.4
-
5
-
-
0028507333
-
HIV Therapy Advances. Update on a Proteinase Inhibitor
-
(a) Vella, S. HIV Therapy Advances. Update on a Proteinase Inhibitor. AIDS 1994, 8 (Suppl. 3), S25-29.
-
(1994)
AIDS
, vol.8
, Issue.3 SUPPL.
-
-
Vella, S.1
-
6
-
-
0028110476
-
Use of Proteinase Inhibitors in Clinical Practice
-
(b) Pollard, R. B. Use of Proteinase Inhibitors in Clinical Practice. Pharmacotherapy 1994, 14, 21S-29S.
-
(1994)
Pharmacotherapy
, vol.14
-
-
Pollard, R.B.1
-
7
-
-
0028222149
-
An Orally Bioavailable Human Immunodeficiency Virus Type-1 Protease Inhibitor
-
(c) Vacca, J. P.; Dorsey, B. D.; Schlief, W. A.; Levin, R. B.; McDaniel, S. L.; Darke, P. L.; Zugay, J.; Quintero, J. C.; Blahy, O. M.; Roth, E.; Sardana, V. V.; Schlabach, A. J.; Graham, P. I.; Condra, J. H.; Gotlib, L.; Holloway, M. k.; Lin, J.; Chen, I.-W.; Ostovic, D.; Anderson, P. S.; Emini, E. A.; Huff, J. R. An Orally Bioavailable Human Immunodeficiency Virus Type-1 Protease Inhibitor. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4096-4100.
-
(1994)
Proc. Natl. Acad. Sci. U.S.A.
, vol.91
, pp. 4096-4100
-
-
Vacca, J.P.1
Dorsey, B.D.2
Schlief, W.A.3
Levin, R.B.4
McDaniel, S.L.5
Darke, P.L.6
Zugay, J.7
Quintero, J.C.8
Blahy, O.M.9
Roth, E.10
Sardana, V.V.11
Schlabach, A.J.12
Graham, P.I.13
Condra, J.H.14
Gotlib, L.15
Holloway, M.K.16
Lin, J.17
Chen, I.-W.18
Ostovic, D.19
Anderson, P.S.20
Emini, E.A.21
Huff, J.R.22
more..
-
8
-
-
0028811974
-
Viral Dynamics in Human Immunodeficiency Virus Type 1 Infection
-
(d) Wei, X.; Ghosh, S. K.; Taylor, M. E.; Johnson, V. A.; Emini, E. A.; Deutsch, P.; Lifson, J. d.; Bonhoeffer, S.; Nowak, M. A.; Hahn, B. H.; Saag, M. S.; Shaw, G. M. Viral Dynamics in Human Immunodeficiency Virus Type 1 Infection. Nature 1995, 373, 117-122.
-
(1995)
Nature
, vol.373
, pp. 117-122
-
-
Wei, X.1
Ghosh, S.K.2
Taylor, M.E.3
Johnson, V.A.4
Emini, E.A.5
Deutsch, P.6
Lifson, J.D.7
Bonhoeffer, S.8
Nowak, M.A.9
Hahn, B.H.10
Saag, M.S.11
Shaw, G.M.12
-
9
-
-
0028968902
-
ABT-538 is a Potent Inhibitor of Human Immunodeficiency Virus Protease with High Oral Bioavailability in Humans
-
(e) Kempf, D.; Marsh, K. C.; Denissen, J. F.; McDonald, E.; Vasavanonda, S.; Flentge, C. A.; Green, B. G.; Fino, L.; Park, C. H.; Kong, X.-P.; Wideburg, N. E.; Saldivar, A.; Ruiz, L.; Kati, W. M.; Sham, H. L.; Robins, T.; Stewart, K. D.; Hsu, A.; Plattner, J. J.; Leonard, J. M.; Norbeck, D. W. ABT-538 is a Potent Inhibitor of Human Immunodeficiency Virus Protease with High Oral Bioavailability in Humans. Proc. Natl. Acad. Sci. U.S.A 1995, 92, 2484-2488.
-
(1995)
Proc. Natl. Acad. Sci. U.S.A
, vol.92
, pp. 2484-2488
-
-
Kempf, D.1
Marsh, K.C.2
Denissen, J.F.3
McDonald, E.4
Vasavanonda, S.5
Flentge, C.A.6
Green, B.G.7
Fino, L.8
Park, C.H.9
Kong, X.-P.10
Wideburg, N.E.11
Saldivar, A.12
Ruiz, L.13
Kati, W.M.14
Sham, H.L.15
Robins, T.16
Stewart, K.D.17
Hsu, A.18
Plattner, J.J.19
Leonard, J.M.20
Norbeck, D.W.21
more..
-
10
-
-
0028874048
-
Rapid Turnover of Plasma Virions and CD4 Lymphocytes in HIV-1 Infection
-
(f) Ho, D. D.; Neumann, A. U.; Perelson, A. S.; Chen, W.; Leonard, J. M.; Markowitz, M. Rapid Turnover of Plasma Virions and CD4 Lymphocytes in HIV-1 Infection. Nature 1995, 373, 123-126.
-
(1995)
Nature
, vol.373
, pp. 123-126
-
-
Ho, D.D.1
Neumann, A.U.2
Perelson, A.S.3
Chen, W.4
Leonard, J.M.5
Markowitz, M.6
-
11
-
-
0029644513
-
Safety and Activity of Saquinavir in HIV Infection
-
(g) Kitchen, V. S.; Skinner, C.; Ariyoshi, K.; Lane, E. A.; Duncan, I. B.; Burckhardt, J.; Burger, H. U.; Bragman, K.; Pinching, A. J.; Weber, J. N. Safety and Activity of Saquinavir in HIV Infection. Lancet 1995, 345, 952-955.
-
(1995)
Lancet
, vol.345
, pp. 952-955
-
-
Kitchen, V.S.1
Skinner, C.2
Ariyoshi, K.3
Lane, E.A.4
Duncan, I.B.5
Burckhardt, J.6
Burger, H.U.7
Bragman, K.8
Pinching, A.J.9
Weber, J.N.10
-
12
-
-
0027218692
-
Structure-based Inhibitors of HIV-1 Protease
-
(a) Wlodawer, A.; Erickson, J. W. Structure-based Inhibitors of HIV-1 Protease. Annu. Rev. Biochem. 1993, 62, 543-585.
-
(1993)
Annu. Rev. Biochem.
, vol.62
, pp. 543-585
-
-
Wlodawer, A.1
Erickson, J.W.2
-
13
-
-
16044375105
-
Crystal Structures of HIV-1 Protease-inhibitor Complexes
-
(b) Appelt, K. Crystal Structures of HIV-1 Protease-inhibitor Complexes. Perspect. Drug Discovery Des. 1993, 1, 23-48.
-
(1993)
Perspect. Drug Discovery Des.
, vol.1
, pp. 23-48
-
-
Appelt, K.1
-
14
-
-
0025196082
-
2 Symmetric Inhibitors of HIV Protease
-
2 Symmetric Inhibitors of HIV Protease. J. Med. Chem. 1990, 33, 2687-2689. For reviews, see:
-
(1990)
J. Med. Chem.
, vol.33
, pp. 2687-2689
-
-
Kempf, D.J.1
Norbeck, D.W.2
Codacovi, L.M.3
Wang, X.C.4
Kohlbrenner, W.E.5
Wideburg, N.E.6
Paul, D.A.7
Knigge, M.F.8
Vasavanonda, S.9
Craig-Kennard, A.10
Saldivar, A.11
Rosen-brook, W.12
Clement, J.J.13
Plattner, J.J.14
Erickson, J.15
-
16
-
-
0001903028
-
The Complexities of AIDS: An Assessment of the HIV Protease as a Therapeutic Target
-
(c) Tomasselli, A. G.; Howe, W. J.; Sawyer, T. K.; Wlodawer, A.; Heinrikson, R. L. The Complexities of AIDS: An Assessment of the HIV Protease as a Therapeutic Target. Chim. Oggi 1991, 6-27.
-
(1991)
Chim. Oggi
, pp. 6-27
-
-
Tomasselli, A.G.1
Howe, W.J.2
Sawyer, T.K.3
Wlodawer, A.4
Heinrikson, R.L.5
-
17
-
-
0025952925
-
HIV Protease: A Novel Chemotherapeutic Target for AIDS
-
(d) Huff, J. R. HIV Protease: A Novel Chemotherapeutic Target for AIDS. J. Med. Chem. 1991, 34, 2305-2314.
-
(1991)
J. Med. Chem.
, vol.34
, pp. 2305-2314
-
-
Huff, J.R.1
-
18
-
-
0026561407
-
Recent Advances in the Design of HIV Proteinase Inhibitors
-
(e) Martin, J. A. Recent Advances in the Design of HIV Proteinase Inhibitors. Antiviral Res. 1992, 17, 265-278.
-
(1992)
Antiviral Res.
, vol.17
, pp. 265-278
-
-
Martin, J.A.1
-
20
-
-
0000213878
-
Progress in the Discovery of Orally Bioavailable Inhibitors of HIV Protease
-
(g) Kempf, D. J. Progress in the Discovery of Orally Bioavailable Inhibitors of HIV Protease. Perspect. Drug Discovery Des. 1994, 2, 427-436.
-
(1994)
Perspect. Drug Discovery Des.
, vol.2
, pp. 427-436
-
-
Kempf, D.J.1
-
21
-
-
0028971801
-
Progress in Anti-HIV Structure-based Drug Design
-
(h) Gait, M. J.; Karn, J. Progress in Anti-HIV Structure-based Drug Design. TiBTECH 1995, 13, 430-437.
-
(1995)
TiBTECH
, vol.13
, pp. 430-437
-
-
Gait, M.J.1
Karn, J.2
-
22
-
-
0028986487
-
Targeting HIV-1 Protease. A Test of Drug-design Methodologies
-
(i) West, M. L.; Fairlie, D. P. Targeting HIV-1 Protease. A Test of Drug-design Methodologies. TiPS 1995, 16, 67-74.
-
(1995)
TiPS
, vol.16
, pp. 67-74
-
-
West, M.L.1
Fairlie, D.P.2
-
23
-
-
0029011730
-
Toward Improved Anti-HIV Chemotherapy: Therapeutic Strategies for Intervention with HIV Infections
-
(j) De Clercq, E. Toward Improved Anti-HIV Chemotherapy: Therapeutic Strategies for Intervention with HIV Infections. J. Med. Chem. 1995, 38, 2491-2517.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 2491-2517
-
-
De Clercq, E.1
-
24
-
-
77956866252
-
Antiviral Agents
-
(k) Boehme, R. E.; Borthwick, A. D.; Wyatt, P. G. Antiviral Agents. Annu. Rep. Med. Chem. 1995, 30, 139-149.
-
(1995)
Annu. Rep. Med. Chem.
, vol.30
, pp. 139-149
-
-
Boehme, R.E.1
Borthwick, A.D.2
Wyatt, P.G.3
-
25
-
-
0028843163
-
Characterization of Human Immunodeficiency Virus Type 1 Mutants with Decreased Sensitivity to Proteinase Inhibitor Ro 31-8959
-
(a) Jacobsen, H.; Yasargil, K.; Winslow, D. L.; Craig, J. C.; Krohn, A.; Duncan, I. B.; Mous, J. Characterization of Human Immunodeficiency Virus Type 1 Mutants with Decreased Sensitivity to Proteinase Inhibitor Ro 31-8959. Virology 1995, 206, 527-534.
-
(1995)
Virology
, vol.206
, pp. 527-534
-
-
Jacobsen, H.1
Yasargil, K.2
Winslow, D.L.3
Craig, J.C.4
Krohn, A.5
Duncan, I.B.6
Mous, J.7
-
26
-
-
0028854676
-
Selection and Analysis of Human Immunodeficiency Virus Type 1 Variants with Increased Resistance to ABT-538, a Novel Protease Inhibitor
-
(b) Markowitz, M. M.; Mo, H.; Kempf, D. J.; Norbeck, D. W.; Bhat, T. N.; Erickson, J. W.; Ho, D. Selection and Analysis of Human Immunodeficiency Virus Type 1 Variants with Increased Resistance to ABT-538, a Novel Protease Inhibitor. J. Virol. 1995, 69, 701-706.
-
(1995)
J. Virol.
, vol.69
, pp. 701-706
-
-
Markowitz, M.M.1
Mo, H.2
Kempf, D.J.3
Norbeck, D.W.4
Bhat, T.N.5
Erickson, J.W.6
Ho, D.7
-
27
-
-
0028943992
-
In Vivo Emergence of HIV-1 Variants Resistant to Multiple Protease Inhibitors
-
(c) Condra, J. H.; Schlelf, W. A.; Blahy, O. M.; Gabryelski, L. J.; Graham, D. J.; Quintero, J. C.; Rhodes, A.; Bobbins, H. L.; Roth, E.; Shivaprakash, M.; Titus, D.; Yang, T.; Teppler, H.; Squires, K. E.; Deutsch, P. J.; Emini, E. A. In Vivo Emergence of HIV-1 Variants Resistant to Multiple Protease Inhibitors. Nature 1995, 374, 569-571.
-
(1995)
Nature
, vol.374
, pp. 569-571
-
-
Condra, J.H.1
Schlelf, W.A.2
Blahy, O.M.3
Gabryelski, L.J.4
Graham, D.J.5
Quintero, J.C.6
Rhodes, A.7
Bobbins, H.L.8
Roth, E.9
Shivaprakash, M.10
Titus, D.11
Yang, T.12
Teppler, H.13
Squires, K.E.14
Deutsch, P.J.15
Emini, E.A.16
-
28
-
-
0029563229
-
Development of Drug Resistance to HIV-1 Protease Inhibitors
-
(d) Ridky, T.; Leis, J. Development of Drug Resistance to HIV-1 Protease Inhibitors. J. Biol. Chem. 1995, 270, 29621-29623.
-
(1995)
J. Biol. Chem.
, vol.270
, pp. 29621-29623
-
-
Ridky, T.1
Leis, J.2
-
29
-
-
0025225682
-
X-ray Crystallographic Structure of a Complex between a Synthetic Protease of Human Immunodeficiency Virus 1 and a Substrate-based Hydroxyethylamine Inhibitor
-
(a) Swain, A. L.; Miller, M. M.; Green, J.; Rich, D. H.; Schneider, J.; Kent, S. B. H.; Wlodawer, A. X-ray Crystallographic Structure of a Complex Between a Synthetic Protease of Human Immunodeficiency Virus 1 and a Substrate-based Hydroxyethylamine Inhibitor. Proc. Natl. Acad. Sci. U.S.A. 1990, 87, 8805-8809.
-
(1990)
Proc. Natl. Acad. Sci. U.S.A.
, vol.87
, pp. 8805-8809
-
-
Swain, A.L.1
Miller, M.M.2
Green, J.3
Rich, D.H.4
Schneider, J.5
Kent, S.B.H.6
Wlodawer, A.7
-
30
-
-
0024992935
-
2 Symmetric Inhibitor Complexed to HIV-1 Protease
-
2 Symmetric Inhibitor Complexed to HIV-1 Protease. Science 1990, 249, 527-532.
-
(1990)
Science
, vol.249
, pp. 527-532
-
-
Erickson, J.1
-
31
-
-
0026323860
-
The Crystal Structures of Recombinant Glycosylated Human Renin Alone and in Complex with a Transition State Analog Inhibitor
-
(a) Rahuel, J.; Priestle, J. P.; Grutter, M. G. The Crystal Structures of Recombinant Glycosylated Human Renin Alone and in Complex with a Transition State Analog Inhibitor. J. Struct. Biol. 1991, 107, 227-236.
-
(1991)
J. Struct. Biol.
, vol.107
, pp. 227-236
-
-
Rahuel, J.1
Priestle, J.P.2
Grutter, M.G.3
-
32
-
-
0026683982
-
X-ray Analyses of Peptide-Inhibitor Complexes Define the Structural Basis of Specificity for Human and Mouse Renins
-
(b) Dhanaraj, V.; Dealwis, C. G.; Frazao, C.; Badasso, M.; Sibanda, B. L.; Tickle, I. J.; Cooper, J. B.; Driessen, H. P. C.; Newman, M.; Aguilar, C.; Wood, S. P.; Blundell, T. L.; Hobart, P. M.; Geoghegan, K. F.; Ammirati, M. J.; Danley, D. E.; O'Connor, B. A.; Hoover, D. J. X-ray Analyses of Peptide-Inhibitor Complexes Define the Structural Basis of Specificity for Human and Mouse Renins. Nature 1992, 357, 466-472.
-
(1992)
Nature
, vol.357
, pp. 466-472
-
-
Dhanaraj, V.1
Dealwis, C.G.2
Frazao, C.3
Badasso, M.4
Sibanda, B.L.5
Tickle, I.J.6
Cooper, J.B.7
Driessen, H.P.C.8
Newman, M.9
Aguilar, C.10
Wood, S.P.11
Blundell, T.L.12
Hobart, P.M.13
Geoghegan, K.F.14
Ammirati, M.J.15
Danley, D.E.16
O'Connor, B.A.17
Hoover, D.J.18
-
33
-
-
34447487903
-
De Novo Design and Discovery of Potent, Nonpeptidal HIV-1 Protease Inhibitors
-
Mar. 28-Apr 2, Division of Med. Chem., No. 96
-
(a) Lam, P. Y. S.; Eyermann, C. J.; Hodge, C. N.; Jadhav, P. K.; Ru, Y.; Bacheler, L. T.; Meek, J. L.; Otto, M. J.; Rayner, M. M.; Wong, N. Y.; Chang, C. H.; Wever, P. C.; Jackson, D. A.; Sharpe, T. R.; Erickson-Viitanen, S. De Novo Design and Discovery of Potent, Nonpeptidal HIV-1 Protease Inhibitors. 205th ACS National Meeting, Mar. 28-Apr 2, 1993; Division of Med. Chem., No. 96.
-
(1993)
205th ACS National Meeting
-
-
Lam, P.Y.S.1
Eyermann, C.J.2
Hodge, C.N.3
Jadhav, P.K.4
Ru, Y.5
Bacheler, L.T.6
Meek, J.L.7
Otto, M.J.8
Rayner, M.M.9
Wong, N.Y.10
Chang, C.H.11
Wever, P.C.12
Jackson, D.A.13
Sharpe, T.R.14
Erickson-Viitanen, S.15
-
34
-
-
9544244531
-
-
PCT Patent Application WO 9307128, 1993
-
(b) Lam, P. Y. S.; Eyermann, C. J.; Hodge, C. N.; Jadhav, P. K.; Delucca, G. V. Substituted Cyclic Carbonyls and Derivatives Thereof Useful as Retroviral Protease Inhibitors. PCT Patent Application WO 9307128, 1993.
-
Substituted Cyclic Carbonyls and Derivatives Thereof Useful As Retroviral Protease Inhibitors
-
-
Lam, P.Y.S.1
Eyermann, C.J.2
Hodge, C.N.3
Jadhav, P.K.4
Delucca, G.V.5
-
35
-
-
0028057975
-
Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors
-
(c) Lam, P. Y. S.; Jadhav, P. K.; Eyermann, C. J.; Hodge, C. N.; Ru, Y.; Bacheler, L. T.; Meek, J. L.; Otto, M. J.; Rayner, M. M.; Wong, N. Y.; Chang, C. H.; Wever, P. C.; Jackson, D. A.; Sharpe, T. R.; Erickson-Vitanen, S. Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors. Science 1994, 263, 380-384.
-
(1994)
Science
, vol.263
, pp. 380-384
-
-
Lam, P.Y.S.1
Jadhav, P.K.2
Eyermann, C.J.3
Hodge, C.N.4
Ru, Y.5
Bacheler, L.T.6
Meek, J.L.7
Otto, M.J.8
Rayner, M.M.9
Wong, N.Y.10
Chang, C.H.11
Wever, P.C.12
Jackson, D.A.13
Sharpe, T.R.14
Erickson-Vitanen, S.15
-
37
-
-
9544239096
-
-
U.S. Patent 5,294,720, Mar. 15, 1994
-
(b) Jadhav, P. K.; McGee, L. R.; Shenvi, A.; Hodge, C. N. 1,4-Diamine-2,3-dihydroxybutanes. U.S. Patent 5,294,720, Mar. 15, 1994.
-
1,4-Diamine-2,3-dihydroxybutanes
-
-
Jadhav, P.K.1
McGee, L.R.2
Shenvi, A.3
Hodge, C.N.4
-
38
-
-
9544229025
-
-
To be published
-
(a) Eyermann, C. J.; et al. To be published.
-
-
-
Eyermann, C.J.1
-
39
-
-
9544254607
-
Molecular Modelling in the Discovery and Optimization of Lead Compounds
-
Chiu, W., Ed.; Oxford Press: Oxford
-
(b) Hodge, C. N.; Straatsma, T. P.; McCammon, J. A.; Wlodawer, A. Molecular Modelling in the Discovery and Optimization of Lead Compounds. In Structural Biology of Viruses; Chiu, W., Ed.; Oxford Press: Oxford, 1996.
-
(1996)
Structural Biology of Viruses
-
-
Hodge, C.N.1
Straatsma, T.P.2
McCammon, J.A.3
Wlodawer, A.4
-
40
-
-
9544242147
-
Nonpeptide Cyclic Urea Inhibitors of HIV Protease
-
(c) Comment by Klunder, J. M. Nonpeptide Cyclic Urea Inhibitors of HIV Protease. Chemtracts-Org. Chem. 1994, 7, 82-87.
-
(1994)
Chemtracts-Org. Chem.
, vol.7
, pp. 82-87
-
-
Klunder, J.M.1
-
41
-
-
0028228418
-
The Entropic Cost of Bound Water in Crystals and Biomolecules
-
Dunitz, J. D. The Entropic Cost of Bound Water in Crystals and Biomolecules. Science 1994, 264, 670.
-
(1994)
Science
, vol.264
, pp. 670
-
-
Dunitz, J.D.1
-
42
-
-
84985545870
-
Preorganization-From Solvents to Spherands
-
(a) Cram, D. J. Preorganization-From Solvents to Spherands. Angew. Chem., Int. Ed. Engl. 1986, 25, 1039-1057.
-
(1986)
Angew. Chem., Int. Ed. Engl.
, vol.25
, pp. 1039-1057
-
-
Cram, D.J.1
-
43
-
-
0024279870
-
The Design of Molecular Hosts, Guests and Their Complexes
-
(b) Cram, D. J. The Design of Molecular Hosts, Guests and Their Complexes. Science 1988, 240, 760-767.
-
(1988)
Science
, vol.240
, pp. 760-767
-
-
Cram, D.J.1
-
44
-
-
0028904424
-
Evaluation of Physicochemical Parameters Important to the Oral Bioavailability of Peptide-like Compounds: Implications for the Synthesis of Renin Inhibitors
-
(a) Hamilton, H. W.; Steinbaugh, B. A.; Stewart, B. H.; Chan, O. H.; Schmid, H. L.; Schroeder, R.; Ryan, M. J.; Keiser, J.; Taylor, M. D.; Blankley, C. J.; Kaltenbronn, J. S.; Wright, J.; Hicks, J. Evaluation of Physicochemical Parameters Important to the Oral Bioavailability of Peptide-like Compounds: Implications for the Synthesis of Renin Inhibitors. J. Med. Chem. 1995, 38, 1446-1455.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 1446-1455
-
-
Hamilton, H.W.1
Steinbaugh, B.A.2
Stewart, B.H.3
Chan, O.H.4
Schmid, H.L.5
Schroeder, R.6
Ryan, M.J.7
Keiser, J.8
Taylor, M.D.9
Blankley, C.J.10
Kaltenbronn, J.S.11
Wright, J.12
Hicks, J.13
-
45
-
-
0028846226
-
Crystal Structure of HIV-1 Protease in complex with VX-478, a Potent and Orally bioavailable Inhibitor of the Enzyme
-
(b) Kim, E. E.; Baker, C. T.; Dwyer, M. D.; Murcko, M. A.; Rao, B. G.; Tung, R. D.; Navia, M. A. Crystal Structure of HIV-1 Protease in complex with VX-478, a Potent and Orally bioavailable Inhibitor of the Enzyme. J. Am. Chem. Soc. 1995, 117, 1181-1182.
-
(1995)
J. Am. Chem. Soc.
, vol.117
, pp. 1181-1182
-
-
Kim, E.E.1
Baker, C.T.2
Dwyer, M.D.3
Murcko, M.A.4
Rao, B.G.5
Tung, R.D.6
Navia, M.A.7
-
47
-
-
33748542524
-
Allylic Strain in Six-Membered Rings
-
(a) Johnson, F. Allylic Strain in Six-Membered Rings. Chem. Rev. 1968, 68, 375-413.
-
(1968)
Chem. Rev.
, vol.68
, pp. 375-413
-
-
Johnson, F.1
-
48
-
-
0026640040
-
Flexible Molecules with Defined Shape-Conformational Design
-
(b) Hoffmann, R. W. Flexible Molecules with Defined Shape-Conformational Design. Angew. Chem., Int. Ed. Engl. 1992, 31, 1124-1134.
-
(1992)
Angew. Chem., Int. Ed. Engl.
, vol.31
, pp. 1124-1134
-
-
Hoffmann, R.W.1
-
50
-
-
32744459401
-
Oxidation of Alcohols by "Activated" Dimethylsulfoxide. A Preparative, Steric and Mechanistic Study
-
Omura, K.; Swern, D. Oxidation of Alcohols by "Activated" Dimethylsulfoxide. A Preparative, Steric and Mechanistic Study. Tetrahedron 1978, 34, 1651-1660.
-
(1978)
Tetrahedron
, vol.34
, pp. 1651-1660
-
-
Omura, K.1
Swern, D.2
-
51
-
-
0000550365
-
Intermolecular Pinacol Cross Coupling of Electronically Similar Aldehydes. An Efficient and Stereoselective Synthesis of 1,2-Diols Employing a Practical Vanadium(II) Reagent
-
(a) Freuidenberger, J. H.; Konradi, A. W.; Pedersen, S. F. Intermolecular Pinacol Cross Coupling of Electronically Similar Aldehydes. An Efficient and Stereoselective Synthesis of 1,2-Diols Employing a Practical Vanadium(II) Reagent. J. Am. Chem. Soc. 1989, 111, 8014-8016.
-
(1989)
J. Am. Chem. Soc.
, vol.111
, pp. 8014-8016
-
-
Freuidenberger, J.H.1
Konradi, A.W.2
Pedersen, S.F.3
-
52
-
-
0026460702
-
2-Symmetric Diamino Alcohols and Diols for Use in HIV Protease Inhibitors
-
2-Symmetric Diamino Alcohols and Diols for Use in HIV Protease Inhibitors. J. Org. Chem. 1992, 57, 5692-5700.
-
(1992)
J. Org. Chem.
, vol.57
, pp. 5692-5700
-
-
Kempf, D.J.1
Sowin, T.J.2
Doherty, E.M.3
Hannick, S.M.4
Codavoci, L.5
Henry, R.F.6
Green, B.E.7
Spanton, S.G.8
Norbeck, D.W.9
-
54
-
-
0028260973
-
Potency and Selectivity of Inhibition of Human Immunodeficiency Virus Protease by a Small Nonpeptide Cyclic Urea, DMP323
-
Erickson-Viitanen, S.; Klabe, R. M.; Cawood, P. G.; O'Neal, P. L.; Meek, J. L. Potency and Selectivity of Inhibition of Human Immunodeficiency Virus Protease by a Small Nonpeptide Cyclic Urea, DMP323. Antimicrob. Agents Chemother. 1994, 38, 1628-1634.
-
(1994)
Antimicrob. Agents Chemother.
, vol.38
, pp. 1628-1634
-
-
Erickson-Viitanen, S.1
Klabe, R.M.2
Cawood, P.G.3
O'Neal, P.L.4
Meek, J.L.5
-
55
-
-
0028235440
-
An Assay for HIV RNA in Infected Cell Lysates, and Its Use for the Rapid Evaluation of Antiviral Efficacy
-
Bacheler, L. T.; Paul, M.; Jadhav, P. K.; Otto, M.; Stone, B.; Miller, J. An Assay for HIV RNA in Infected Cell Lysates, and Its Use for the Rapid Evaluation of Antiviral Efficacy. Antiviral Chem. Chemother. 1994, 5 (2), 111-121.
-
(1994)
Antiviral Chem. Chemother.
, vol.5
, Issue.2
, pp. 111-121
-
-
Bacheler, L.T.1
Paul, M.2
Jadhav, P.K.3
Otto, M.4
Stone, B.5
Miller, J.6
-
56
-
-
9544229024
-
-
note
-
18 column and methanol/water eluant.
-
-
-
-
57
-
-
0028059153
-
A Pharmacokinetic Evaluation of HIV Protease Inhibitors, Cyclic Ureas, in Rats and Dogs
-
Wong, N. Y.; Burcham, D. L.; Saxton, P. L.; Erickson-Viitanen, S.; Grubb, M. F.; Quon, C. Y.; Huang, S.-M. A Pharmacokinetic Evaluation of HIV Protease Inhibitors, Cyclic Ureas, in Rats and Dogs. Biopharm. Drug Dispos. 1994, 15, 535-544.
-
(1994)
Biopharm. Drug Dispos.
, vol.15
, pp. 535-544
-
-
Wong, N.Y.1
Burcham, D.L.2
Saxton, P.L.3
Erickson-Viitanen, S.4
Grubb, M.F.5
Quon, C.Y.6
Huang, S.-M.7
-
58
-
-
34447487589
-
-
Manuscript in preparation
-
The complete macromolecular crystallographic method is described in detail in: Chang, C. H.; Schadt, M. C.; Lewandowski, F. A.; DeLoskey, R.; Duke, J.; Calabrese, J. C.; Lam, P. Y. S.; Jadhav, P. K.; Eyermann, C. J.; Hodge, C. N.; Weber, P. C. Three Dimensional Structures of the HIV-1 Protease Complexed with Novel Non-Peptide, Cyclic Urea-Containing Inhibitors. Manuscript in preparation.
-
Three Dimensional Structures of the HIV-1 Protease Complexed with Novel Non-Peptide, Cyclic Urea-Containing Inhibitors
-
-
Chang, C.H.1
Schadt, M.C.2
Lewandowski, F.A.3
DeLoskey, R.4
Duke, J.5
Calabrese, J.C.6
Lam, P.Y.S.7
Jadhav, P.K.8
Eyermann, C.J.9
Hodge, C.N.10
Weber, P.C.11
-
59
-
-
0028221902
-
NMR Evidence for the Displacement of a Conserved Interior Water Molecule in HIV Protease by a Non-Peptide Cyclic Urea-Based Inhibitor
-
(a) Grzesiek, S.; Bax, A.; Nicholson, L. K.; Yamazaki, T.; Wingfield, P.; Stahl, S. J.; Eyermann, C. J.; Torchia, D. A.; Hodge, C. N.; Lam, P. Y. S.; Jadhav, P. K.; Chang, C.-H. NMR Evidence for the Displacement of a Conserved Interior Water Molecule in HIV Protease by a Non-Peptide Cyclic Urea-Based Inhibitor. J. Am. Chem. Soc. 1994, 116, 1581-1582.
-
(1994)
J. Am. Chem. Soc.
, vol.116
, pp. 1581-1582
-
-
Grzesiek, S.1
Bax, A.2
Nicholson, L.K.3
Yamazaki, T.4
Wingfield, P.5
Stahl, S.J.6
Eyermann, C.J.7
Torchia, D.A.8
Hodge, C.N.9
Lam, P.Y.S.10
Jadhav, P.K.11
Chang, C.-H.12
-
60
-
-
0028114966
-
NMR and X-ray Evidence That the HIV Protease Catalytic Aspartyl Groups Are Protonated in the Complex Formed by the Protease and a Non-Peptide Cycyclic Urea-Based Inhibitor
-
(b) Yamazaki, T.; Nicholson, L. K.; Torchia, D. A.; Wingfield, P.; Stahl, S. J.; Kaufman, J. D.; Eyermann, C. J.; Hodge, C. N.; Lam, P. Y. S.; Ru, Y.; Jadhav, P. K.; Chang, C.-H.; Weber, P. C. NMR and X-ray Evidence That the HIV Protease Catalytic Aspartyl Groups Are Protonated in the Complex Formed by the Protease and a Non-Peptide Cycyclic Urea-Based Inhibitor. J. Am. Chem. Soc. 1994, 16, 10791-10792.
-
(1994)
J. Am. Chem. Soc.
, vol.16
, pp. 10791-10792
-
-
Yamazaki, T.1
Nicholson, L.K.2
Torchia, D.A.3
Wingfield, P.4
Stahl, S.J.5
Kaufman, J.D.6
Eyermann, C.J.7
Hodge, C.N.8
Lam, P.Y.S.9
Ru, Y.10
Jadhav, P.K.11
Chang, C.-H.12
Weber, P.C.13
-
61
-
-
0028921302
-
Flexibility and Function in HIV-1 Protease
-
(c) Nicholson, L. K.; Yamazaki, T.; Torchia, D. A.; Grzesiek, S.; Bax, A.; Stahl, S. J.; Kaufman, J. D.; Wingfield, P. T.; Lam, P. Y. S.; Jadhav, P. K.; Hodge, C. N.; Domaille, P. J.; Chang, C.-H. Flexibility and Function in HIV-1 Protease. Struct. Biol. 1995, 2 274-280.
-
(1995)
Struct. Biol.
, vol.2
, pp. 274-280
-
-
Nicholson, L.K.1
Yamazaki, T.2
Torchia, D.A.3
Grzesiek, S.4
Bax, A.5
Stahl, S.J.6
Kaufman, J.D.7
Wingfield, P.T.8
Lam, P.Y.S.9
Jadhav, P.K.10
Hodge, C.N.11
Domaille, P.J.12
Chang, C.-H.13
-
62
-
-
9044228016
-
Three Dimensional Solution Structure of the HIV-1 Protease Complexed with DMP323, a Novel Cyclic Urea-type Inhibitor, Determined by Nuclear Magnetic Resonce Spectroscopy
-
(d) Yamazaki, T.; Hinck, A. P.; Wang, Y.-X.; Nicholson, L. K.; Torchia, D. A.; Wingfield, P.; Stahl, S. J.; Kaufman, J. D.; Chang, C.-H.; Domaille, P. J.; Lam, P. Y. S. Three Dimensional Solution Structure of the HIV-1 Protease Complexed with DMP323, a Novel Cyclic Urea-type Inhibitor, Determined by Nuclear Magnetic Resonce Spectroscopy. Protein Sci. 1996, 5, 495-506.
-
(1996)
Protein Sci.
, vol.5
, pp. 495-506
-
-
Yamazaki, T.1
Hinck, A.P.2
Wang, Y.-X.3
Nicholson, L.K.4
Torchia, D.A.5
Wingfield, P.6
Stahl, S.J.7
Kaufman, J.D.8
Chang, C.-H.9
Domaille, P.J.10
Lam, P.Y.S.11
-
63
-
-
0027731531
-
Nonpeptide HIV Protease Inhibitors Designed to Replace a Bound Water
-
(a) Chenera, B.; DesJarlais, R. L.; Finkelstein, J. A.; Eggleston, D. S.; Meek, T. D.; Tomaszek, T. A.; Dryer, G. B. Nonpeptide HIV Protease Inhibitors Designed to Replace a Bound Water. Bioorg. Med. Chem. Lett. 1993, 3, 2717-2722.
-
(1993)
Bioorg. Med. Chem. Lett.
, vol.3
, pp. 2717-2722
-
-
Chenera, B.1
DesJarlais, R.L.2
Finkelstein, J.A.3
Eggleston, D.S.4
Meek, T.D.5
Tomaszek, T.A.6
Dryer, G.B.7
-
64
-
-
9544221385
-
-
EP 589322-A1, 1994
-
(b) Wild, H.; Hansen, J.; Lautz, J.; Paessens, A. Preparation of 5-Oxodibenzo-(a,d)cyclohepta-1,4-diene Derivatives as Antiretroviral Agents. EP 589322-A1, 1994.
-
Preparation of 5-Oxodibenzo-(a,d)cyclohepta-1,4-diene Derivatives As Antiretroviral Agents
-
-
Wild, H.1
Hansen, J.2
Lautz, J.3
Paessens, A.4
-
65
-
-
0028287967
-
De Novo Design of Nonpeptidic HIV-1 Protease Inhibitors: Incorporation of Structural Water
-
(c) Randad, R. S.; Pan, W.; Gulnik, S. V.; Burt, S.; Erickson, J. W. De Novo Design of Nonpeptidic HIV-1 Protease Inhibitors: Incorporation of Structural Water. Bioorg. Med. Chem. Lett. 1994, 4, 1247-1252.
-
(1994)
Bioorg. Med. Chem. Lett.
, vol.4
, pp. 1247-1252
-
-
Randad, R.S.1
Pan, W.2
Gulnik, S.V.3
Burt, S.4
Erickson, J.W.5
-
66
-
-
0028094959
-
Novel Series of Achiral, Low Molecular Weight, and Potent HIV-1 Protese Inhibitors
-
(d) Vara Prasad, J. V. N.; et al. Novel Series of Achiral, Low Molecular Weight, and Potent HIV-1 Protese Inhibitors. J. Am. Chem. Soc. 1994, 116, 6989-6990.
-
(1994)
J. Am. Chem. Soc.
, vol.116
, pp. 6989-6990
-
-
Vara Prasad, J.V.N.1
-
67
-
-
0027942206
-
Non-Peptide-Based Inhibitors of Human Immunodeficiency Virus-1 Protease
-
(e) Peyman, A.; Stahl, W.; Wagner, K.; Ruppert, D.; Budt, K.-H. Non-Peptide-Based Inhibitors of Human Immunodeficiency Virus-1 Protease. Bioorg. Med. Chem. Lett. 1994, 4, 2601-2604.
-
(1994)
Bioorg. Med. Chem. Lett.
, vol.4
, pp. 2601-2604
-
-
Peyman, A.1
Stahl, W.2
Wagner, K.3
Ruppert, D.4
Budt, K.-H.5
-
68
-
-
0029091140
-
Synthesis of 8-Membered Cyclic Sulfamides: Novel HIV-1 Protease Inhibitors
-
(f) Jadhav, P. K.; Woerner, F. J. Synthesis of 8-Membered Cyclic Sulfamides: Novel HIV-1 Protease Inhibitors. Tetrahedron Lett. 1995, 36, 6383-6386.
-
(1995)
Tetrahedron Lett.
, vol.36
, pp. 6383-6386
-
-
Jadhav, P.K.1
Woerner, F.J.2
-
69
-
-
13344295092
-
A Novel, Picomolar Inhibitor of Human Immunodeficiency Virus Type 1 Protease
-
(g) Sham, H. L.; Zhao, C.; Stewart, K. D.; Betebenner, D. A.; Lin, S.; Park, C. H.; Kong, X.-P.; Rosenbrook, W., Jr.; Herrin, T.; Madigan, D.; Vasavanonda, S.; Lyons, N.; Molla, A.; Saldivar, A.; Marsh, K. C.; McDonald, E.; Wideburg, N. E.; Denissen, J. F.; Robins, T.; Kempf, D. J.; Plattner, J. J.; Norbeck, D. W. A Novel, Picomolar Inhibitor of Human Immunodeficiency Virus Type 1 Protease. J. Med. Chem. 1996, 39, 392-397.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 392-397
-
-
Sham, H.L.1
Zhao, C.2
Stewart, K.D.3
Betebenner, D.A.4
Lin, S.5
Park, C.H.6
Kong, X.-P.7
Rosenbrook Jr., W.8
Herrin, T.9
Madigan, D.10
Vasavanonda, S.11
Lyons, N.12
Molla, A.13
Saldivar, A.14
Marsh, K.C.15
McDonald, E.16
Wideburg, N.E.17
Denissen, J.F.18
Robins, T.19
Kempf, D.J.20
Plattner, J.J.21
Norbeck, D.W.22
more..
-
70
-
-
0029896691
-
Preparation and SAR of Novel P1/P1′ Substituted Cyclic Urea Based HIV-1 Protease Inhibitors
-
(h) Nugiel, D. A.; Jacobs, K.; Worley, T.; Patel, M.; Kaltenbach, R. F., III; Meyer, D. T.; Jadhav, P. K.; De Lucca, G. V.; Smyser, T. E.; Klabe, R. M.; Bacheler, L. T.; Rayner, M. M.; Seitz, S. P. Preparation and SAR of Novel P1/P1′ Substituted Cyclic Urea Based HIV-1 Protease Inhibitors. J. Med. Chem. 1996, 39, 2156-2169.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 2156-2169
-
-
Nugiel, D.A.1
Jacobs, K.2
Worley, T.3
Patel, M.4
Kaltenbach III, R.F.5
Meyer, D.T.6
Jadhav, P.K.7
De Lucca, G.V.8
Smyser, T.E.9
Klabe, R.M.10
Bacheler, L.T.11
Rayner, M.M.12
Seitz, S.P.13
-
71
-
-
0028128838
-
A Novel Nonpeptide HIV-1 Protease Inhibitor: Elucidation of the Binding Mode and Its Application in the Design of Related Analogs
-
(a) Lunney, E. A.; Hagen, S. E.; Domagala, J. M.; Humblet, C.; Kosinski, J.; Tait, B. D.; Warmus, J. S.; Wilson, M.; Ferguson, D.; Hupe, D.; Tummino, P. T.; Baldwin, E. T.; Bhat, T. N.; Liu, B.; Erickson, J. W. A Novel Nonpeptide HIV-1 Protease Inhibitor: Elucidation of the Binding Mode and Its Application in the Design of Related Analogs. J. Med. Chem. 1994, 37, 2664-2677.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 2664-2677
-
-
Lunney, E.A.1
Hagen, S.E.2
Domagala, J.M.3
Humblet, C.4
Kosinski, J.5
Tait, B.D.6
Warmus, J.S.7
Wilson, M.8
Ferguson, D.9
Hupe, D.10
Tummino, P.T.11
Baldwin, E.T.12
Bhat, T.N.13
Liu, B.14
Erickson, J.W.15
-
72
-
-
0028094959
-
Novel Series of Achiral, Low Molecular Weight, and Potent HIV-1 Protease Inhibitors
-
(b) Prasad, J. V. N. V.; Para, K. S.; Lunney, E. A.; Ortwine, D. F.; Dunbar, J. B.; Ferguson, D.; Tummino, P. J.; Hupe, D.; Tait, B. D.; Domagala, J. M.; Humblet, C.; Bhat, T. N.; Liu, B.; Guerin, D. M. A.; Baldwin, E. T.; Erickson, J. W.; Sawyer, T. K. Novel Series of Achiral, Low Molecular Weight, and Potent HIV-1 Protease Inhibitors. J. Am. Chem. Soc. 1994, 116, 6989-6990.
-
(1994)
J. Am. Chem. Soc.
, vol.116
, pp. 6989-6990
-
-
Prasad, J.V.N.V.1
Para, K.S.2
Lunney, E.A.3
Ortwine, D.F.4
Dunbar, J.B.5
Ferguson, D.6
Tummino, P.J.7
Hupe, D.8
Tait, B.D.9
Domagala, J.M.10
Humblet, C.11
Bhat, T.N.12
Liu, B.13
Guerin, D.M.A.14
Baldwin, E.T.15
Erickson, J.W.16
Sawyer, T.K.17
-
73
-
-
0028946741
-
Nonpeptidic Potent HIV-1 Protease Inhibitors: (4-Hydroxy-6-phenyl-2-oxo-2H-pyran-3-yl)thiomethanes That Span P1-P2′ Subsites in a Unique Mode of Active Site Binding
-
(c) Prasad, J. V. N. V.; Para, K. S.; Tummino, P. J.; Ferguson, D.; McQuade, T. J.; Lunney, E. A.; Rapundalo, S. T.; Batley, B. L.; Hingorani, G.; Domagala, J. M.; Gracheck, S. J.; Bhat, T. N.; Liu, B.; Baldwin, E. T.; Erickson, J. W.; Sawyer, T. K. Nonpeptidic Potent HIV-1 Protease Inhibitors: (4-Hydroxy-6-phenyl-2-oxo-2H-pyran-3-yl)thiomethanes That Span P1-P2′ Subsites in a Unique Mode of Active Site Binding. J. Med. Chem. 1995, 38, 898-905.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 898-905
-
-
Prasad, J.V.N.V.1
Para, K.S.2
Tummino, P.J.3
Ferguson, D.4
McQuade, T.J.5
Lunney, E.A.6
Rapundalo, S.T.7
Batley, B.L.8
Hingorani, G.9
Domagala, J.M.10
Gracheck, S.J.11
Bhat, T.N.12
Liu, B.13
Baldwin, E.T.14
Erickson, J.W.15
Sawyer, T.K.16
-
74
-
-
0028028221
-
Structure-Based Design of HIV Protease Inhibitors: 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Nonpeptidic Inhibitors
-
(d) Thaisrivongs, S.; Tomich, P. K.; Watenpaugh, K. D.; Chong, K.-T.; Howe, W. J.; Yang, C.-P.; Strohbach, J. W.; Turner, S. R.; McGrath, J. P.; Bohanon, M. J.; Lynn, J. C.; Mulichak, A. M.; Spinelli, P. A.; Hinshaw, R. R.; Pagano, P. J.; Moon, J. B.; Ruwart, M. J.; Wilkinson, K. F.; Rush, B. D.; Zipp, G. L.; Dalga, R. J.; Schwende, F. J.; Howard, G. M.; Padbury, G. E.; Toth, L. N.; Zhao, Z.; Koeplinger, K. A.; Kakuk, T. J.; Cole, S. L.; Zaya, R. M.; Piper, R. C.; Jeffrey, P. Structure-Based Design of HIV Protease Inhibitors: 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Nonpeptidic Inhibitors. J. Med. Chem. 1994, 37, 3200-3204.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 3200-3204
-
-
Thaisrivongs, S.1
Tomich, P.K.2
Watenpaugh, K.D.3
Chong, K.-T.4
Howe, W.J.5
Yang, C.-P.6
Strohbach, J.W.7
Turner, S.R.8
McGrath, J.P.9
Bohanon, M.J.10
Lynn, J.C.11
Mulichak, A.M.12
Spinelli, P.A.13
Hinshaw, R.R.14
Pagano, P.J.15
Moon, J.B.16
Ruwart, M.J.17
Wilkinson, K.F.18
Rush, B.D.19
Zipp, G.L.20
Dalga, R.J.21
Schwende, F.J.22
Howard, G.M.23
Padbury, G.E.24
Toth, L.N.25
Zhao, Z.26
Koeplinger, K.A.27
Kakuk, T.J.28
Cole, S.L.29
Zaya, R.M.30
Piper, R.C.31
Jeffrey, P.32
more..
-
75
-
-
0029024605
-
Use of Medium-Sized Cycloalkyl Rings to Enhance Secondary Binding: Discovery of a New Class of Human Immunodeficiency Virus (HIV) Proteases Inhibitors
-
(e) Romines, K. R.; Watenpaugh, K. D.; Tomich, P. K.; Howe, W. J.; Morris, J. K.; Lovasz, K. D.; Mulichak, A. M.; Finzel, B. C.; Lynn, J. C.; Horng, M.-M.; Schwende, F. J.; Ruwart, M. J.; Zipp, G. L.; Chong, K.-T.; Dolak, L. A.; Toth, L. N.; Howard, G. M.; Rush, B. D.; Wilkinson, K. F.; Possert, P. L.; Dalga, R. J.; Hinshaw, R. R. Use of Medium-Sized Cycloalkyl Rings to Enhance Secondary Binding: Discovery of a New Class of Human Immunodeficiency Virus (HIV) Proteases Inhibitors. J. Med. Chem. 1995, 38, 1884-1891.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 1884-1891
-
-
Romines, K.R.1
Watenpaugh, K.D.2
Tomich, P.K.3
Howe, W.J.4
Morris, J.K.5
Lovasz, K.D.6
Mulichak, A.M.7
Finzel, B.C.8
Lynn, J.C.9
Horng, M.-M.10
Schwende, F.J.11
Ruwart, M.J.12
Zipp, G.L.13
Chong, K.-T.14
Dolak, L.A.15
Toth, L.N.16
Howard, G.M.17
Rush, B.D.18
Wilkinson, K.F.19
Possert, P.L.20
Dalga, R.J.21
Hinshaw, R.R.22
more..
-
76
-
-
0029131933
-
Structure-Based Design of Novel Protease Inhibitors: Carboxamide-Containing 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Potent Nonpeptidic Inhibitors
-
(f) Thaisrivongs, S.; Watenpaugh, K. D.; Howe, W. J.; Tomich, P. K.; Dolak, L. A.; Chong, K.-T.; Tomich, C.-S.; Tomasselli, A. G.; Turner, S. R.; Strohbach, J. W.; Mulichak, A. M.; Janakiraman, M. N.; Moon, J. B.; Lynn, J. C.; Horng, M.-M.; Hinshaw, R. R.; Curry, K. A.; Rothrock, D. J. Structure-Based Design of Novel Protease Inhibitors: Carboxamide-Containing 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Potent Nonpeptidic Inhibitors. J. Med. Chem. 1995, 38, 3624-3637.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 3624-3637
-
-
Thaisrivongs, S.1
Watenpaugh, K.D.2
Howe, W.J.3
Tomich, P.K.4
Dolak, L.A.5
Chong, K.-T.6
Tomich, C.-S.7
Tomasselli, A.G.8
Turner, S.R.9
Strohbach, J.W.10
Mulichak, A.M.11
Janakiraman, M.N.12
Moon, J.B.13
Lynn, J.C.14
Horng, M.-M.15
Hinshaw, R.R.16
Curry, K.A.17
Rothrock, D.J.18
-
77
-
-
0028842736
-
Structure-Based Design of Nonpeptidic HIV Protease Inhibitors from a Cyclooctylpyranone Lead Structure
-
(g) Romines, K. R.; Watenpaugh, K. D.; Howe, W. J.; Tomich, P. K.; Lovasz, K. D.; Morris, J. K.; Janakiraman, M. N.; Lynn, J. C.; Horng, M.-M.; Chong, K.-T.; Hinshaw, R. R.; Dolak, L. A. Structure-Based Design of Nonpeptidic HIV Protease Inhibitors from a Cyclooctylpyranone Lead Structure. J. Med. Chem. 1995, 38, 4463-4473.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 4463-4473
-
-
Romines, K.R.1
Watenpaugh, K.D.2
Howe, W.J.3
Tomich, P.K.4
Lovasz, K.D.5
Morris, J.K.6
Janakiraman, M.N.7
Lynn, J.C.8
Horng, M.-M.9
Chong, K.-T.10
Hinshaw, R.R.11
Dolak, L.A.12
-
78
-
-
34447488119
-
-
Manuscript in preparation
-
Hodge, C. N.; Ru, Y.; Aldrich, P. E.; Lam, P. Y. S.; Jadhav, P. K.; DeLucca, G. V.; Kaltenbach, R. F., III; Chang, C. H.; Fernandez, C. H.; Holler, E. E.; Woerner, F. J.; Calabrese, J. C.; Daneker, W. K.; Emmett, G. C. Calculated and Experimental Conformations of Cyclic Urea Inhibitors of HIV Protease. Manuscript in preparation.
-
Calculated and Experimental Conformations of Cyclic Urea Inhibitors of HIV Protease
-
-
Hodge, C.N.1
Ru, Y.2
Aldrich, P.E.3
Lam, P.Y.S.4
Jadhav, P.K.5
DeLucca, G.V.6
Kaltenbach III, R.F.7
Chang, C.H.8
Fernandez, C.H.9
Holler, E.E.10
Woerner, F.J.11
Calabrese, J.C.12
Daneker, W.K.13
Emmett, G.C.14
-
79
-
-
9544222378
-
-
Small-molecule crystal structures solved by J. C. Calabrese of E. I. DuPont de Nemours & Co. Inc. See Supporting Information for complete methods and coordinates
-
Small-molecule crystal structures solved by J. C. Calabrese of E. I. DuPont de Nemours & Co. Inc. See Supporting Information for complete methods and coordinates.
-
-
-
-
80
-
-
0002134667
-
Effect of Hydrophobic Collapse on Enzyme-Inhibitor Interaction. Implication for the Design of Peptidal Mimetics
-
Testa, B.; Kyburz, E., Fuhrer, W., Giger, R., Eds.; VCH: New York
-
Rich, D. H. Effect of Hydrophobic Collapse on Enzyme-Inhibitor Interaction. Implication for the Design of Peptidal Mimetics. In Perspectives in Medicinal Chemistry; Testa, B.; Kyburz, E., Fuhrer, W., Giger, R., Eds.; VCH: New York, 1993; pp 15-25.
-
(1993)
Perspectives in Medicinal Chemistry
, pp. 15-25
-
-
Rich, D.H.1
-
81
-
-
0027491485
-
Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors
-
(a) Otto, M. J.; Reid, C. D.; Garber, S.; Lam, P. Y. S.; Scarnati, H.; Bacheler, L. T.; Rayner, M. M.; Winslow, D. L. Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors. Antimicrob. Agents Chemother. 1993, 37, 2606-2611.
-
(1993)
Antimicrob. Agents Chemother.
, vol.37
, pp. 2606-2611
-
-
Otto, M.J.1
Reid, C.D.2
Garber, S.3
Lam, P.Y.S.4
Scarnati, H.5
Bacheler, L.T.6
Rayner, M.M.7
Winslow, D.L.8
-
82
-
-
0028232645
-
DMP323, a Nonpeptide Cyclic Urea Inhibitor of Human Immunodeficiency Virus (HIV) Protease, Specifically and Persistently Blocks Intracellular Processing of HIV gag Polyprotein
-
(b) Rayner, M. M.; Cordova, B. C.; Meade, R. P.; Aldrich, P. E.; Jadhav, P. K.; Ru, Y.; Lam, P. Y. S. DMP323, a Nonpeptide Cyclic Urea Inhibitor of Human Immunodeficiency Virus (HIV) Protease, Specifically and Persistently Blocks Intracellular Processing of HIV gag Polyprotein. Antimicrob. Agents Chemother. 1994, 38, 1635-1640.
-
(1994)
Antimicrob. Agents Chemother.
, vol.38
, pp. 1635-1640
-
-
Rayner, M.M.1
Cordova, B.C.2
Meade, R.P.3
Aldrich, P.E.4
Jadhav, P.K.5
Ru, Y.6
Lam, P.Y.S.7
-
83
-
-
0028023629
-
Pharmacokinetics of HIV Protease Inhibitor DMP323 in Rats and Dogs
-
(c) Grubb, M. F.; Wong, Y. N.; Burcham, D. L.; Saxton, P. L.; Quon, C. Y.; Huang, S.-M. Pharmacokinetics of HIV Protease Inhibitor DMP323 in Rats and Dogs. Drug Metab. Dispos. 1994, 22, 709-712.
-
(1994)
Drug Metab. Dispos.
, vol.22
, pp. 709-712
-
-
Grubb, M.F.1
Wong, Y.N.2
Burcham, D.L.3
Saxton, P.L.4
Quon, C.Y.5
Huang, S.-M.6
-
84
-
-
9544231455
-
-
Unpublished data. The metabolic instability of the benzyl alcohol of DMP323 was also of concern
-
Shum, L. I.; Winslow, D. L.; Kornhauser, D. M.; et al. Unpublished data. The metabolic instability of the benzyl alcohol of DMP323 was also of concern.
-
-
-
Shum, L.I.1
Winslow, D.L.2
Kornhauser, D.M.3
-
85
-
-
0030113025
-
DMP450: An Orally Bioavailable Cyclic Urea Inhibitor of the HIV Protease
-
Hodge, C. N.; Aldrich, P. E.; Bacheler, L. T.; Chang, C.-H.; Eyermann, C. J.; Grubb, M. F.; Jackson, D. A.; Jadhav, P. K.; Korant, B.; Lam, P. Y. S.; Maurin, M. B.; Meek, J. L.; Otto, M. J.; Rayner, M. M.; Sharpe, T. R.; Shum, L.; Winslow, D. L.; Erickson-Viitanen, S. DMP450: An Orally Bioavailable Cyclic Urea Inhibitor of the HIV Protease. Chem. Biol. 1996, 3, 301-314. Avid Pharmaceutical Co. (Philadelphia, PA) has recently acquired the option to license DMP450.
-
(1996)
Chem. Biol.
, vol.3
, pp. 301-314
-
-
Hodge, C.N.1
Aldrich, P.E.2
Bacheler, L.T.3
Chang, C.-H.4
Eyermann, C.J.5
Grubb, M.F.6
Jackson, D.A.7
Jadhav, P.K.8
Korant, B.9
Lam, P.Y.S.10
Maurin, M.B.11
Meek, J.L.12
Otto, M.J.13
Rayner, M.M.14
Sharpe, T.R.15
Shum, L.16
Winslow, D.L.17
Erickson-Viitanen, S.18
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