Proteins > Protease
Page last updated: 2024-08-07 17:16:32
Protease
[no definition available]
Synonyms
Research
Bioassay Publications (148)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 77 (52.03) | 18.2507 |
| 2000's | 50 (33.78) | 29.6817 |
| 2010's | 9 (6.08) | 24.3611 |
| 2020's | 12 (8.11) | 2.80 |
Compounds (77)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| haloperidol | Human immunodeficiency virus 1 | IC50 | 125.0000 | 1 | 1 |
| haloperidol | Human immunodeficiency virus 1 | Ki | 50.0500 | 2 | 2 |
| loviride | Human immunodeficiency virus 1 | IC50 | 8.2500 | 1 | 2 |
| nevirapine | Human immunodeficiency virus 1 | IC50 | 23.1003 | 3 | 3 |
| protoporphyrin ix | Human immunodeficiency virus 1 | IC50 | 250.0000 | 2 | 2 |
| sulfamethoxazole | Human immunodeficiency virus 1 | Ki | 0.0101 | 1 | 1 |
| adenosine monophosphate | Human immunodeficiency virus 1 | Ki | 0.0002 | 1 | 1 |
| lawsone | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| zidovudine | Human immunodeficiency virus 1 | IC50 | 12.5112 | 3 | 4 |
| atevirdine | Human immunodeficiency virus 1 | IC50 | 34.9733 | 3 | 3 |
| nelfinavir mesylate | Human immunodeficiency virus 1 | Ki | 0.0020 | 1 | 1 |
| nelfinavir | Human immunodeficiency virus 1 | IC50 | 0.5300 | 1 | 1 |
| nelfinavir | Human immunodeficiency virus 1 | Ki | 0.0164 | 17 | 17 |
| betulinic acid | Human immunodeficiency virus 1 | IC50 | 219.0000 | 1 | 1 |
| calanolide a | Human immunodeficiency virus 1 | IC50 | 3.6000 | 3 | 3 |
| abbott 77003 | Human immunodeficiency virus 1 | Ki | 0.0001 | 1 | 1 |
| l-697661 | Human immunodeficiency virus 1 | IC50 | 8.5270 | 3 | 3 |
| kni 102 | Human immunodeficiency virus 1 | IC50 | 0.0074 | 2 | 2 |
| kni 102 | Human immunodeficiency virus 1 | Ki | 0.0040 | 1 | 1 |
| amprenavir | Human immunodeficiency virus 1 | IC50 | 0.3242 | 5 | 5 |
| amprenavir | Human immunodeficiency virus 1 | Ki | 0.0140 | 33 | 33 |
| bms 186318 | Human immunodeficiency virus 1 | IC50 | 0.1000 | 1 | 1 |
| a 74704 | Human immunodeficiency virus 1 | IC50 | 0.0030 | 3 | 3 |
| a 75925 | Human immunodeficiency virus 1 | IC50 | 0.0002 | 2 | 2 |
| a 76889 | Human immunodeficiency virus 1 | Ki | 0.0001 | 2 | 2 |
| dmp 323 | Human immunodeficiency virus 1 | IC50 | 0.0625 | 2 | 2 |
| dmp 323 | Human immunodeficiency virus 1 | Ki | 0.0003 | 12 | 12 |
| palinavir | Human immunodeficiency virus 1 | IC50 | 0.0060 | 3 | 3 |
| palinavir | Human immunodeficiency virus 1 | Ki | 0.0000 | 2 | 2 |
| lopinavir | Human immunodeficiency virus 1 | IC50 | 0.0250 | 1 | 1 |
| lopinavir | Human immunodeficiency virus 1 | Ki | 0.0007 | 15 | 15 |
| n-acetylseryl-leucyl-asparaginyl(phenylalanyl-hydroxyethylamino-prolyl)isoleucyl-valyl methyl ester | Human immunodeficiency virus 1 | IC50 | 0.0342 | 1 | 2 |
| n-acetylseryl-leucyl-asparaginyl(phenylalanyl-hydroxyethylamino-prolyl)isoleucyl-valyl methyl ester | Human immunodeficiency virus 1 | Ki | 0.0036 | 5 | 6 |
| atazanavir | Human immunodeficiency virus 1 | IC50 | 0.0040 | 1 | 1 |
| atazanavir | Human immunodeficiency virus 1 | Ki | 0.0003 | 8 | 8 |
| dmp 450 | Human immunodeficiency virus 1 | Ki | 0.0003 | 8 | 8 |
| l 734005 | Human immunodeficiency virus 1 | IC50 | 0.8380 | 3 | 3 |
| uic-94003 | Human immunodeficiency virus 1 | Ki | 0.0011 | 1 | 1 |
| darunavir | Human immunodeficiency virus 1 | IC50 | 0.0630 | 6 | 6 |
| darunavir | Human immunodeficiency virus 1 | Ki | 0.0178 | 31 | 31 |
| sc 52151 | Human immunodeficiency virus 1 | IC50 | 0.0060 | 1 | 1 |
| ritonavir | Human immunodeficiency virus 1 | Ki | 0.0090 | 14 | 14 |
| adam ii | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| xv 638 | Human immunodeficiency virus 1 | Ki | 0.0000 | 4 | 4 |
| saquinavir | Human immunodeficiency virus 1 | IC50 | 0.0217 | 16 | 16 |
| saquinavir | Human immunodeficiency virus 1 | Ki | 0.0171 | 25 | 25 |
| skf 107457 | Human immunodeficiency virus 1 | Ki | 0.0111 | 2 | 2 |
| a 76928 | Human immunodeficiency virus 1 | Ki | 0.0053 | 2 | 2 |
| xk 263 | Human immunodeficiency virus 1 | Ki | 0.0003 | 3 | 3 |
| je 2147 | Human immunodeficiency virus 1 | Ki | 0.0003 | 1 | 1 |
| mvt 101 | Human immunodeficiency virus 1 | IC50 | 1.9000 | 1 | 1 |
| mvt 101 | Human immunodeficiency virus 1 | Ki | 0.7781 | 2 | 2 |
| 85548e | Human immunodeficiency virus 1 | Ki | 0.0010 | 1 | 1 |
| kni-727 | Human immunodeficiency virus 1 | Ki | 0.0014 | 1 | 1 |
| l 737126 | Human immunodeficiency virus 1 | IC50 | 0.0875 | 4 | 4 |
| l 739594 | Human immunodeficiency virus 1 | IC50 | 0.0669 | 1 | 2 |
| grl 98065 | Human immunodeficiency virus 1 | Ki | 0.0021 | 4 | 4 |
| bevirimat | Human immunodeficiency virus 1 | IC50 | 171.0000 | 1 | 1 |
| costatolide | Human immunodeficiency virus 1 | IC50 | 91.7500 | 2 | 2 |
| dmp 850 | Human immunodeficiency virus 1 | Ki | 0.0000 | 1 | 1 |
| dpc 961 | Human immunodeficiency virus 1 | IC50 | 0.0310 | 1 | 1 |
| pl 100 | Human immunodeficiency virus 1 | IC50 | 0.0005 | 1 | 1 |
| r-82913 | Human immunodeficiency virus 1 | IC50 | 15.7103 | 3 | 3 |
| grl 02031 | Human immunodeficiency virus 1 | Ki | 0.0007 | 4 | 4 |
| cerulenin | Human immunodeficiency virus 1 | IC50 | 2.5000 | 1 | 1 |
| indinavir sulfate | Human immunodeficiency virus 1 | IC50 | 0.0349 | 33 | 33 |
| indinavir sulfate | Human immunodeficiency virus 1 | Ki | 0.0129 | 27 | 27 |
| indinavir sulfate | Human immunodeficiency virus 1 | IC50 | 0.0004 | 1 | 1 |
| l 685434 | Human immunodeficiency virus 1 | IC50 | 0.0003 | 9 | 9 |
| l 689502 | Human immunodeficiency virus 1 | IC50 | 0.0004 | 2 | 2 |
| l 682679 | Human immunodeficiency virus 1 | IC50 | 0.0006 | 4 | 4 |
| pepstatin | Human immunodeficiency virus 1 | Ki | 1.1867 | 4 | 4 |
| u 75875 | Human immunodeficiency virus 1 | IC50 | 0.3755 | 2 | 2 |
| u 75875 | Human immunodeficiency virus 1 | Ki | 0.0014 | 5 | 5 |
| streptomyces pepsin inhibitor | Human immunodeficiency virus 1 | Ki | 0.0252 | 3 | 3 |
| l 754394 | Human immunodeficiency virus 1 | IC50 | 0.0004 | 1 | 1 |
| brecanavir | Human immunodeficiency virus 1 | Ki | 0.0000 | 1 | 1 |
| PF-00835231 | Human immunodeficiency virus 1 | IC50 | 10.0000 | 1 | 1 |
| g 52 | Human immunodeficiency virus 1 | Ki | 0.0095 | 5 | 5 |
| warfarin | Human immunodeficiency virus 1 | IC50 | 30.0000 | 1 | 1 |
| phenprocoumon | Human immunodeficiency virus 1 | IC50 | 1.0000 | 1 | 1 |
| phenprocoumon | Human immunodeficiency virus 1 | Ki | 0.7002 | 4 | 4 |
| tipranavir | Human immunodeficiency virus 1 | IC50 | 0.0300 | 2 | 2 |
| tipranavir | Human immunodeficiency virus 1 | Ki | 0.0003 | 2 | 3 |
| ethyl biscoumacetate | Human immunodeficiency virus 1 | IC50 | 100.0000 | 1 | 1 |
| nsc 158393 | Human immunodeficiency virus 1 | IC50 | 1.7000 | 1 | 1 |
| pd 178390 | Human immunodeficiency virus 1 | IC50 | 0.0006 | 2 | 2 |
| pd 178390 | Human immunodeficiency virus 1 | Ki | 0.0001 | 2 | 2 |
| pnu 103017 | Human immunodeficiency virus 1 | IC50 | 2.0000 | 2 | 2 |
| pnu 103017 | Human immunodeficiency virus 1 | Ki | 0.0009 | 4 | 4 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| sulfamethoxazole | Human immunodeficiency virus 1 | Kd | 0.5770 | 1 | 1 |
| adenosine monophosphate | Human immunodeficiency virus 1 | Kd | 0.0011 | 1 | 1 |
| zidovudine | Human immunodeficiency virus 1 | EC50 | 0.1260 | 1 | 1 |
| nelfinavir | Human immunodeficiency virus 1 | Kd | 0.0016 | 2 | 2 |
| abbott 77003 | Human immunodeficiency virus 1 | EC50 | 0.0700 | 1 | 1 |
| amprenavir | Human immunodeficiency virus 1 | Kd | 0.0011 | 1 | 1 |
| a 76889 | Human immunodeficiency virus 1 | EC50 | 0.0600 | 1 | 1 |
| dmp 323 | Human immunodeficiency virus 1 | Kd | 0.0038 | 1 | 1 |
| lopinavir | Human immunodeficiency virus 1 | Kd | 0.0001 | 1 | 1 |
| atazanavir | Human immunodeficiency virus 1 | Kd | 0.0004 | 1 | 1 |
| ritonavir | Human immunodeficiency virus 1 | Kd | 0.0006 | 2 | 2 |
| saquinavir | Human immunodeficiency virus 1 | Kd | 0.0227 | 3 | 3 |
| a 76928 | Human immunodeficiency virus 1 | EC50 | 0.2800 | 1 | 1 |
| indinavir sulfate | Human immunodeficiency virus 1 | Kd | 0.0011 | 2 | 2 |
| u 75875 | Human immunodeficiency virus 1 | Kd | 0.0005 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| flavaspidic acid | Human immunodeficiency virus 1 | ID50 | 26.0000 | 1 | 1 |
| hydrocortisone hemisuccinate | Human immunodeficiency virus 1 | ID50 | 27.0000 | 1 | 1 |
| efavirenz | Human immunodeficiency virus 1 | IC90 | 3.7260 | 4 | 4 |
| nelfinavir | Human immunodeficiency virus 1 | ED50 | 0.5520 | 5 | 5 |
| nelfinavir | Human immunodeficiency virus 1 | Km | 24.6143 | 7 | 7 |
| l-697661 | Human immunodeficiency virus 1 | IC90 | 0.8000 | 1 | 1 |
| amprenavir | Human immunodeficiency virus 1 | IC90 | 0.0690 | 3 | 3 |
| amprenavir | Human immunodeficiency virus 1 | K | 0.1780 | 1 | 1 |
| zidovudine triphosphate | Human immunodeficiency virus 1 | ID50 | 54.0000 | 1 | 1 |
| dmp 323 | Human immunodeficiency virus 1 | IC90 | 0.1048 | 2 | 2 |
| atazanavir | Human immunodeficiency virus 1 | ED50 | 0.0014 | 1 | 1 |
| atazanavir | Human immunodeficiency virus 1 | ED90 | 0.0030 | 1 | 1 |
| dmp 450 | Human immunodeficiency virus 1 | IC90 | 0.1225 | 2 | 2 |
| darunavir | Human immunodeficiency virus 1 | ID50 | 0.0014 | 1 | 1 |
| darunavir | Human immunodeficiency virus 1 | K | 0.0410 | 1 | 1 |
| ritonavir | Human immunodeficiency virus 1 | ED50 | 0.8140 | 5 | 5 |
| ritonavir | Human immunodeficiency virus 1 | IC90 | 0.1253 | 3 | 3 |
| xv 638 | Human immunodeficiency virus 1 | IC90 | 0.0042 | 1 | 1 |
| saquinavir | Human immunodeficiency virus 1 | ED50 | 0.0241 | 6 | 6 |
| saquinavir | Human immunodeficiency virus 1 | ED90 | 0.0100 | 1 | 1 |
| saquinavir | Human immunodeficiency virus 1 | IC90 | 0.0127 | 2 | 2 |
| saquinavir | Human immunodeficiency virus 1 | IC95 | 0.0220 | 2 | 2 |
| saquinavir | Human immunodeficiency virus 1 | ID50 | 0.0180 | 1 | 1 |
| l 739594 | Human immunodeficiency virus 1 | IC95 | 0.2973 | 2 | 3 |
| dpc 961 | Human immunodeficiency virus 1 | IC90 | 0.4500 | 5 | 5 |
| grl 02031 | Human immunodeficiency virus 1 | K | 0.9600 | 1 | 1 |
| dpc 083 | Human immunodeficiency virus 1 | IC90 | 0.7048 | 5 | 5 |
| indinavir sulfate | Human immunodeficiency virus 1 | IC90 | 0.0570 | 3 | 3 |
| indinavir sulfate | Human immunodeficiency virus 1 | IC95 | 0.0250 | 2 | 2 |
| indinavir sulfate | Human immunodeficiency virus 1 | IC95 | 0.0500 | 1 | 1 |
| l 685434 | Human immunodeficiency virus 1 | IC95 | 0.4000 | 2 | 2 |
| l 682679 | Human immunodeficiency virus 1 | IC95 | 6.0000 | 2 | 2 |
| l 754394 | Human immunodeficiency virus 1 | IC95 | 0.0060 | 1 | 1 |
| g 52 | Human immunodeficiency virus 1 | K | 0.0395 | 1 | 1 |
| tipranavir | Human immunodeficiency virus 1 | ED50 | 300.0000 | 1 | 1 |
| tipranavir | Human immunodeficiency virus 1 | ED90 | 0.1000 | 1 | 1 |
| tipranavir | Human immunodeficiency virus 1 | IC90 | 0.1167 | 3 | 3 |
| nsc 158393 | Human immunodeficiency virus 1 | ID50 | 1.7000 | 2 | 2 |
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.
Journal of medicinal chemistry, , Mar-04, Volume: 37, Issue:5, 1994
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.
Journal of medicinal chemistry, , Mar-04, Volume: 37, Issue:5, 1994
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Specific inhibition of HIV-1 protease by boronated porphyrins.
Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease.
Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching.
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching.
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor.
Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 9, Issue:6, 1999
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 9, Issue:6, 1999
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease.
Journal of medicinal chemistry, , Nov-21, Volume: 40, Issue:24, 1997
Journal of medicinal chemistry, , Nov-21, Volume: 40, Issue:24, 1997
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.
Bioorganic & medicinal chemistry letters, , Jul-08, Volume: 12, Issue:13, 2002
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.
Bioorganic & medicinal chemistry letters, , Jul-08, Volume: 12, Issue:13, 2002
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents.
Journal of medicinal chemistry, , Mar-01, Volume: 39, Issue:5, 1996
Journal of medicinal chemistry, , Mar-01, Volume: 39, Issue:5, 1996
Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers.
Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Three-dimensional QSAR of human immunodeficiency virus (I) protease inhibitors. 1. A CoMFA study employing experimentally-determined alignment rules.
Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
Intriguing structure-activity relations underlie the potent inhibition of HIV protease by norstatine-based peptides.
Journal of medicinal chemistry, , Apr-03, Volume: 35, Issue:7, 1992
Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
Intriguing structure-activity relations underlie the potent inhibition of HIV protease by norstatine-based peptides.
Journal of medicinal chemistry, , Apr-03, Volume: 35, Issue:7, 1992
Recent applications of seven-membered rings in drug design.
Bioorganic & medicinal chemistry, , 03-01, Volume: 57, 2022
Room Temperature Neutron Crystallography of Drug Resistant HIV-1 Protease Uncovers Limitations of X-ray Structural Analysis at 100 K.
Journal of medicinal chemistry, , 03-09, Volume: 60, Issue:5, 2017
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance.
Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 15, Issue:15, 2005
Optimization of pyrrolidinone based HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Hydroxyethylene sulfones as a new scaffold to address aspartic proteases: design, synthesis, and structural characterization.
Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres.
Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease.
Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Design and synthesis of novel conformationally restricted HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 8, Issue:24, 1998
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.
Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 8, Issue:24, 1998
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Bioorganic & medicinal chemistry, , 03-01, Volume: 57, 2022
Room Temperature Neutron Crystallography of Drug Resistant HIV-1 Protease Uncovers Limitations of X-ray Structural Analysis at 100 K.
Journal of medicinal chemistry, , 03-09, Volume: 60, Issue:5, 2017
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance.
Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 15, Issue:15, 2005
Optimization of pyrrolidinone based HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Hydroxyethylene sulfones as a new scaffold to address aspartic proteases: design, synthesis, and structural characterization.
Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres.
Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease.
Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Design and synthesis of novel conformationally restricted HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 8, Issue:24, 1998
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.
Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 8, Issue:24, 1998
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching.
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Synthesis and anti-HIV activities of symmetrical N1,N3-dibenzyl-2-hydroxy-propane derivatives.
Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Cyclopropane-derived peptidomimetics. Design, synthesis, evaluation, and structure of novel HIV-1 protease inhibitors.
Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Cyclopropane-derived peptidomimetics. Design, synthesis, evaluation, and structure of novel HIV-1 protease inhibitors.
Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease.
Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.
Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.
Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.
Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities.
Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.
Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas.
Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Preparation and structure-activity relationship of novel P1/P1'-substituted cyclic urea-based human immunodeficiency virus type-1 protease inhibitors.
Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease.
Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.
Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.
Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.
Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities.
Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.
Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas.
Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Preparation and structure-activity relationship of novel P1/P1'-substituted cyclic urea-based human immunodeficiency virus type-1 protease inhibitors.
Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors.
Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere.
Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere.
Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach.
European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach.
European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.
Journal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase.
Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere.
Journal of medicinal chemistry, , Volume: 34, Issue:11, 1991
Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes.
Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Hydroxyethylamine analogues of the p17/p24 substrate cleavage site are tight-binding inhibitors of HIV protease.
Journal of medicinal chemistry, , Volume: 33, Issue:5, 1990
Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere.
Journal of medicinal chemistry, , Volume: 34, Issue:11, 1991
Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes.
Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Hydroxyethylamine analogues of the p17/p24 substrate cleavage site are tight-binding inhibitors of HIV protease.
Journal of medicinal chemistry, , Volume: 33, Issue:5, 1990
Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach.
European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors.
Journal of medicinal chemistry, , Jan-14, Volume: 42, Issue:1, 1999
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.
Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.
Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.
Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.
Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
Journal of medicinal chemistry, , Jan-14, Volume: 42, Issue:1, 1999
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.
Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.
Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.
Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.
Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.
Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
A kind of HIV-1 protease inhibitors containing phenols with antiviral activity against DRV-resistant variants.
Bioorganic & medicinal chemistry, , 06-15, Volume: 64, 2022
Design, synthesis and biological evaluation of protease inhibitors containing morpholine cores with remarkable potency against both HIV-1 subtypes B and C.
European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Design and evaluation of novel piperidine HIV-1 protease inhibitors with potency against DRV-resistant variants.
European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Design, synthesis and biological evaluation of HIV-1 protease inhibitors with morpholine derivatives as P2 ligands in combination with cyclopropyl as P1' ligand.
Bioorganic & medicinal chemistry letters, , 04-01, Volume: 30, Issue:7, 2020
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Design and biological evaluation of novel HIV-1 protease inhibitors with isopropanol as P1' ligand to enhance binding with S1' subsite.
Bioorganic & medicinal chemistry, , 08-15, Volume: 28, Issue:16, 2020
Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants.
ACS medicinal chemistry letters, , Jun-11, Volume: 11, Issue:6, 2020
Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.
European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.
Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance.
Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Potent new antiviral compound shows similar inhibition and structural interactions with drug resistant mutants and wild type HIV-1 protease.
Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Structure-based design of novel HIV-1 protease inhibitors to combat drug resistance.
Journal of medicinal chemistry, , Aug-24, Volume: 49, Issue:17, 2006
Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M.
Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Structure-based design: synthesis and biological evaluation of a series of novel cycloamide-derived HIV-1 protease inhibitors.
Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.
Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Bioorganic & medicinal chemistry, , 06-15, Volume: 64, 2022
Design, synthesis and biological evaluation of protease inhibitors containing morpholine cores with remarkable potency against both HIV-1 subtypes B and C.
European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Design and evaluation of novel piperidine HIV-1 protease inhibitors with potency against DRV-resistant variants.
European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Design, synthesis and biological evaluation of HIV-1 protease inhibitors with morpholine derivatives as P2 ligands in combination with cyclopropyl as P1' ligand.
Bioorganic & medicinal chemistry letters, , 04-01, Volume: 30, Issue:7, 2020
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Design and biological evaluation of novel HIV-1 protease inhibitors with isopropanol as P1' ligand to enhance binding with S1' subsite.
Bioorganic & medicinal chemistry, , 08-15, Volume: 28, Issue:16, 2020
Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants.
ACS medicinal chemistry letters, , Jun-11, Volume: 11, Issue:6, 2020
Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.
European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.
Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance.
Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Potent new antiviral compound shows similar inhibition and structural interactions with drug resistant mutants and wild type HIV-1 protease.
Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Structure-based design of novel HIV-1 protease inhibitors to combat drug resistance.
Journal of medicinal chemistry, , Aug-24, Volume: 49, Issue:17, 2006
Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M.
Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Structure-based design: synthesis and biological evaluation of a series of novel cycloamide-derived HIV-1 protease inhibitors.
Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.
Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere.
Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution.
Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents.
Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution.
Journal of medicinal chemistry, , Apr-08, Volume: 47, Issue:8, 2004
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents.
Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.
Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Why Some Targets Benefit from beyond Rule of Five Drugs.
Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir.
Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.
Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.
Bioorganic & medicinal chemistry letters, , Jul-08, Volume: 12, Issue:13, 2002
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy.
Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand.
Bioorganic & medicinal chemistry letters, , Apr-21, Volume: 8, Issue:8, 1998
Structure based design: novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Apr-21, Volume: 8, Issue:8, 1998
Comparative binding energy analysis of HIV-1 protease inhibitors: incorporation of solvent effects and validation as a powerful tool in receptor-based drug design.
Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability.
Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.
Journal of medicinal chemistry, , Jan-20, Volume: 38, Issue:2, 1995
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors: heterocyclic ring systems containing P1' and P2' substituents.
Journal of medicinal chemistry, , Oct-28, Volume: 37, Issue:22, 1994
Three-dimensional QSAR of human immunodeficiency virus (I) protease inhibitors. 1. A CoMFA study employing experimentally-determined alignment rules.
Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships.
Journal of medicinal chemistry, , Oct-15, Volume: 36, Issue:21, 1993
Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Apr-02, Volume: 36, Issue:7, 1993
Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands.
Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity.
Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere.
Journal of medicinal chemistry, , Volume: 34, Issue:11, 1991
Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Why Some Targets Benefit from beyond Rule of Five Drugs.
Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir.
Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.
Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.
Bioorganic & medicinal chemistry letters, , Jul-08, Volume: 12, Issue:13, 2002
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy.
Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand.
Bioorganic & medicinal chemistry letters, , Apr-21, Volume: 8, Issue:8, 1998
Structure based design: novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Apr-21, Volume: 8, Issue:8, 1998
Comparative binding energy analysis of HIV-1 protease inhibitors: incorporation of solvent effects and validation as a powerful tool in receptor-based drug design.
Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability.
Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.
Journal of medicinal chemistry, , Jan-20, Volume: 38, Issue:2, 1995
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors: heterocyclic ring systems containing P1' and P2' substituents.
Journal of medicinal chemistry, , Oct-28, Volume: 37, Issue:22, 1994
Three-dimensional QSAR of human immunodeficiency virus (I) protease inhibitors. 1. A CoMFA study employing experimentally-determined alignment rules.
Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships.
Journal of medicinal chemistry, , Oct-15, Volume: 36, Issue:21, 1993
Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Apr-02, Volume: 36, Issue:7, 1993
Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands.
Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity.
Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere.
Journal of medicinal chemistry, , Volume: 34, Issue:11, 1991
Efficient evaluation of binding free energy using continuum electrostatics solvation.
Journal of medicinal chemistry, , Nov-04, Volume: 47, Issue:23, 2004
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Journal of medicinal chemistry, , Nov-04, Volume: 47, Issue:23, 2004
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Design, synthesis, evaluation, and crystallographic-based structural studies of HIV-1 protease inhibitors with reduced response to the V82A mutation.
Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.
Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.
Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.
Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.
Journal of medicinal chemistry, , May-20, Volume: 42, Issue:10, 1999
Journal of medicinal chemistry, , May-20, Volume: 42, Issue:10, 1999
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere.
Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase.
Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere.
Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase.
Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase.
Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.
Journal of medicinal chemistry, , May-20, Volume: 42, Issue:10, 1999
Journal of medicinal chemistry, , May-20, Volume: 42, Issue:10, 1999
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.
Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Nonpeptidal P2 ligands for HIV protease inhibitors: structure-based design, synthesis, and biological evaluation.
Journal of medicinal chemistry, , Aug-16, Volume: 39, Issue:17, 1996
Structure-based design of HIV-1 protease inhibitors: replacement of two amides and a 10 pi-aromatic system by a fused bis-tetrahydrofuran.
Journal of medicinal chemistry, , Aug-05, Volume: 37, Issue:16, 1994
Journal of medicinal chemistry, , Aug-16, Volume: 39, Issue:17, 1996
Structure-based design of HIV-1 protease inhibitors: replacement of two amides and a 10 pi-aromatic system by a fused bis-tetrahydrofuran.
Journal of medicinal chemistry, , Aug-05, Volume: 37, Issue:16, 1994
Potent new antiviral compound shows similar inhibition and structural interactions with drug resistant mutants and wild type HIV-1 protease.
Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents.
Journal of medicinal chemistry, , Mar-01, Volume: 39, Issue:5, 1996
Journal of medicinal chemistry, , Mar-01, Volume: 39, Issue:5, 1996
Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers.
Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors.
Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-acyl aromatic alpha-amino acids.
Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1'-pyrrolidinone ring.
Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1'-pyrrolidinone ring.
Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.
Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M.
Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.
Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold.
Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.
Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 14, Issue:18, 2004
The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 13, Issue:15, 2003
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.
Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.
Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.
Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 13, Issue:15, 2003
Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.
Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.
Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 2003
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.
Bioorganic & medicinal chemistry letters, , May-19, Volume: 13, Issue:10, 2003
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.
Bioorganic & medicinal chemistry letters, , Jul-08, Volume: 12, Issue:13, 2002
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Sep-02, Volume: 12, Issue:17, 2002
A combinatorial library of indinavir analogues and its in vitro and in vivo studies.
Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease.
Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.
Bioorganic & medicinal chemistry letters, , Jul-17, Volume: 10, Issue:14, 2000
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor.
Journal of medicinal chemistry, , Oct-14, Volume: 37, Issue:21, 1994
Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.
Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M.
Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.
Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Feb-23, Volume: 14, Issue:4, 2004
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold.
Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.
Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 14, Issue:18, 2004
The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 13, Issue:15, 2003
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.
Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.
Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.
Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 13, Issue:15, 2003
Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.
Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.
Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 2003
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.
Bioorganic & medicinal chemistry letters, , May-19, Volume: 13, Issue:10, 2003
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.
Bioorganic & medicinal chemistry letters, , Jul-08, Volume: 12, Issue:13, 2002
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
Bioorganic & medicinal chemistry letters, , Sep-02, Volume: 12, Issue:17, 2002
A combinatorial library of indinavir analogues and its in vitro and in vivo studies.
Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Protease inhibitors: current status and future prospects.
Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease.
Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.
Bioorganic & medicinal chemistry letters, , Jul-17, Volume: 10, Issue:14, 2000
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor.
Journal of medicinal chemistry, , Oct-14, Volume: 37, Issue:21, 1994
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.
Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Comparative binding energy analysis of HIV-1 protease inhibitors: incorporation of solvent effects and validation as a powerful tool in receptor-based drug design.
Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.
Journal of medicinal chemistry, , Jan-20, Volume: 38, Issue:2, 1995
3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.
Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors.
Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Comparative binding energy analysis of HIV-1 protease inhibitors: incorporation of solvent effects and validation as a powerful tool in receptor-based drug design.
Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.
Journal of medicinal chemistry, , Jan-20, Volume: 38, Issue:2, 1995
3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.
Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors.
Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.
Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity.
Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity.
Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport.
Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport.
Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
An allosteric modulator of HIV-1 protease shows equipotent inhibition of wild-type and drug-resistant proteases.
Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Crystal-structure-based design and synthesis of novel C-terminal inhibitors of HIV protease.
Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Crystal-structure-based design and synthesis of novel C-terminal inhibitors of HIV protease.
Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities.
Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
Specific inhibition of HIV-1 protease by boronated porphyrins.
Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Journal of medicinal chemistry, , Dec-05, Volume: 45, Issue:25, 2002
Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors.
Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities.
Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
Specific inhibition of HIV-1 protease by boronated porphyrins.
Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Three-dimensional pharmacophores from binding data.
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase.
Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase.
Journal of medicinal chemistry, , Jul-23, Volume: 36, Issue:15, 1993
HIV protease: a novel chemotherapeutic target for AIDS.
Journal of medicinal chemistry, , Volume: 34, Issue:8, 1991
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Journal of medicinal chemistry, , Sep-07, Volume: 43, Issue:18, 2000
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Novel P2 tris-tetrahydrofuran group in antiviral compound 1 (GRL-0519) fills the S2 binding pocket of selected mutants of HIV-1 protease.
Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Novel P2 tris-tetrahydrofuran group in antiviral compound 1 (GRL-0519) fills the S2 binding pocket of selected mutants of HIV-1 protease.
Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors.
Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.
Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 1997
Cycloalkylpyranones and cycloalkyldihydropyrones as HIV protease inhibitors: exploring the impact of ring size on structure-activity relationships.
Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.
Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 1997
Cycloalkylpyranones and cycloalkyldihydropyrones as HIV protease inhibitors: exploring the impact of ring size on structure-activity relationships.
Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties.
Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.
Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.
Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease.
Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease.
Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching.
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
Journal of medicinal chemistry, , Jun-21, Volume: 39, Issue:13, 1996
Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching.
Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters.
Journal of medicinal chemistry, , Jul-05, Volume: 44, Issue:14, 2001
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.
Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.
Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 9, Issue:15, 1999
Journal of medicinal chemistry, , Jul-05, Volume: 44, Issue:14, 2001
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.
Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.
Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 9, Issue:15, 1999
Non-peptidic HIV protease inhibitors: C2-symmetry-based design of bis-sulfonamide dihydropyrones.
Bioorganic & medicinal chemistry letters, , May-19, Volume: 8, Issue:10, 1998
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.
Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 1997
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-22, Volume: 38, Issue:26, 1995
Bioorganic & medicinal chemistry letters, , May-19, Volume: 8, Issue:10, 1998
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.
Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 1997
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Journal of medicinal chemistry, , Oct-25, Volume: 39, Issue:22, 1996
Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors.
Journal of medicinal chemistry, , Dec-22, Volume: 38, Issue:26, 1995