The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
8021917 |
84 |
Three-dimensional pharmacophores from binding data. |
Ciba-Geigy |
11087569 |
37 |
Computational studies on HIV-1 protease inhibitors: influence of calculated inhibitor-enzyme binding affinities on the statistical quality of 3D-QSAR CoMFA models. |
University of Missouri St. Louis |
9526559 |
49 |
Comparative binding energy analysis of HIV-1 protease inhibitors: incorporation of solvent effects and validation as a powerful tool in receptor-based drug design. |
Universidad De Alcal£ |
15993582 |
19 |
Hydrophobicity in the design of P2/P2' tetrahydropyrimidinone HIV protease inhibitors. |
Clarkson University |
10956210 |
85 |
DoMCoSAR: a novel approach for establishing the docking mode that is consistent with the structure-activity relationship. Application to HIV-1 protease inhibitors and VEGF receptor tyrosine kinase inhibitors. |
Eli Lilly |
8523405 |
176 |
3D-quantitative structure-activity relationships of human immunodeficiency virus type-1 proteinase inhibitors: comparative molecular field analysis of 2-heterosubstituted statine derivatives-implications for the design of novel inhibitors. |
Sandoz Forschungsinstitut Ges.M.B.H. |
8035428 |
30 |
Three-dimensional quantitative structure-activity relationship of human immunodeficiency virus (I) protease inhibitors. 2. Predictive power using limited exploration of alternate binding modes. |
Washington University |
8277496 |
77 |
Three-dimensional QSAR of human immunodeficiency virus (I) protease inhibitors. 1. A CoMFA study employing experimentally-determined alignment rules. |
Washington University |
12419382 |
51 |
Six-membered cyclic ureas as HIV-1 protease inhibitors: a QSAR study based on CODESSA PRO approach. Quantitative structure-activity relationships. |
University of Florida |
| 25 |
Synthesis and antiviral activity of a novel class of HIV-1 protease inhibitors containing a heterocyclic P1-P2 amide bond isostere |
TBA |
17964171 |
3 |
Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir. |
Sapienza University of Rome |
16458505 |
2 |
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385. |
Glaxosmithkline |
16509598 |
22 |
Microwave-accelerated synthesis of P1'-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold. |
Uppsala University |
15771466 |
46 |
Development of low molecular weight HIV-1 protease dimerization inhibitors. |
Purdue University |
15537350 |
54 |
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
Uppsala University |
15261290 |
19 |
A unidirectional crosslinking strategy for HIV-1 protease dimerization inhibitors. |
Purdue University |
15056001 |
4 |
A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution. |
Academy of Sciences of The Czech Republic |
15027855 |
30 |
Countering cooperative effects in protease inhibitors using constrained beta-strand-mimicking templates in focused combinatorial libraries. |
The University of Queensland |
14613322 |
12 |
Dimerization inhibitors of HIV-1 protease based on a bicyclic guanidinium subunit. |
Universidad Aut£Noma De Madrid |
12459011 |
94 |
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors. |
Uppsala University |
11462972 |
93 |
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
Universita' Degli Studi Di Salerno |
11428926 |
37 |
4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters. |
Pfizer |
10753465 |
8 |
Conformational selection of inhibitors and substrates by proteolytic enzymes: implications for drug design and polypeptide processing. |
University of Queensland |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
11000004 |
16 |
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease. |
The University of Queensland |
10978186 |
45 |
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors. |
Merck Research Laboratories |
10821707 |
26 |
Modeling of the inhibition of retroviral integrases by styrylquinoline derivatives. |
Cnrs Umr 8532 |
9632374 |
3 |
Optimizing the binding of fullerene inhibitors of the HIV-1 protease through predicted increases in hydrophobic desolvation. |
University of California |
9397180 |
4 |
Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. |
Agouron Pharmaceuticals |
9258349 |
12 |
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex. |
University of Pennsylvania |
8691444 |
105 |
Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease. |
National Cancer Institute-Bethesda |
8164249 |
46 |
Application of the three-dimensional structures of protein target molecules in structure-based drug design. |
Abbott Laboratories |
8295217 |
7 |
Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. |
Upjohn Laboratories |
8478908 |
22 |
Inhibitors of the protease from human immunodeficiency virus: synthesis, enzyme inhibition, and antiviral activity of a series of compounds containing the dihydroxyethylene transition-state isostere. |
Upjohn Laboratories |
8355256 |
11 |
Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities. |
Upjohn |
8340918 |
4 |
Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase. |
Harvard University |
1560443 |
32 |
Intriguing structure-activity relations underlie the potent inhibition of HIV protease by norstatine-based peptides. |
Syntex Research |
1433192 |
27 |
New hydroxyethylamine HIV protease inhibitors that suppress viral replication. |
University of Wisconsin-Madison |
1527792 |
55 |
Specific inhibition of HIV-1 protease by boronated porphyrins. |
University of California |
1875334 |
16 |
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. |
Upjohn |
1875332 |
33 |
HIV protease: a novel chemotherapeutic target for AIDS. |
Merck Sharp and Dohme Research Laboratories |
1766005 |
5 |
Examination of HIV-1 protease secondary structure specificity using conformationally constrained inhibitors. |
University of Illinois |
1956054 |
27 |
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere. |
Roche Products |
15006369 |
7 |
Crucial amides for dimerization inhibitors of HIV-1 protease. |
Purdue University |
12067556 |
8 |
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds. |
University College Dublin |
11212098 |
25 |
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase. |
Dupont Pharmaceuticals |
11591519 |
20 |
Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase. |
University of Toledo |
11549448 |
2 |
Design and synthesis of new inhibitors of HIV-1 protease dimerization with conformationally constrained templates. |
Kyoto Pharmaceutical University |
10386929 |
10 |
The sulfonimidamide as a novel transition state analog for aspartic acid and metallo proteases. |
The University of Kansas |
9871524 |
10 |
Structure based design: novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors. |
University of Illinois At Chicago |
9873718 |
12 |
Restricting the flexibility of crosslinked, interfacial peptide inhibitors of HIV-1 protease. |
Purdue University |
| 35 |
Structure-activity relationships for macrocyclic peptidomimetic inhibitors of HIV-1 protease |
TBA |
| 37 |
Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability properties |
TBA |
| 8 |
Phosphonamidates and phosphonamidate esters as HIV-1 protease inhibitors |
TBA |
| 1 |
Lack of stereospecificity in the binding of the P2 amino acid of ritonavir to HIV protease |
TBA |
| 5 |
Synthesis and evaluation of delta lactams as nonpeptide HIV-protease inhibitors |
TBA |
| 14 |
Synthesis and evaluation of imidazolidinones as nonpeptide HIV-protease inhibitors |
TBA |
| 20 |
Synthesis and pharmacological evaluation of sulfone substituted HIV protease inhibitors |
TBA |
| 10 |
Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres |
TBA |
| 2 |
Synthesis of 7-membered cyclic hydroxyguanidines: Novel HIV-1 protease inhibitors |
TBA |
| 28 |
Functionalized aliphatic P2/P2′ analogs of HIV-1 protease inhibitor DMP323 |
TBA |
| 3 |
Cyclic urea HIV protease inhibitors containing alkynyl- and alkenyl-tethered heterocycles in the P2 region |
TBA |
| 25 |
6-Phenyl-6-alkylamido-5,6-dihydro-2H-pyran-2-ones: novel HIV protease inhibitors |
TBA |
| 6 |
Design, synthesis, and characterization of dipeptide isostere containing cis-epoxide for the irreversible inactivation of HIV protease |
TBA |
| 7 |
β-Methanesulfonyl-L-valine as a novel, unnatural amino acid surrogate for P2 in the design of HIV protease inhibitors. |
TBA |
| 18 |
(Hydroxyethyl) sulfonamide HIV-1 Protease inhibitors: Identification of the 2-methylbenzoyl moiety at P-2 |
TBA |
| 7 |
Synthesis and activity of conformationally-constrained macrocyclic norstatine-based inhibitors of HIV protease |
TBA |
| 23 |
Potent cyclic urea HIV protease inhibitors with benzofused heterocycles as P2/P2′ groups |
TBA |
| 8 |
Design and synthesis of novel, pseudo C2 symmetric inhibitors of HIV protease |
TBA |
| 15 |
Aromatic P1 replacements for the highly potent HIV-1 protease inhibitor CRIXIVAN® |
TBA |
| 11 |
Synthesis of (+)-biotin derivatives as HIV-1 protease inhibitors |
TBA |
| 37 |
Nonpeptidic HIV protease inhibitors: 3-(S-benzyl substituted)-4-hydroxy-6-(phenyl substituted)-2H-pyran-2-one with an inverse mode of binding |
TBA |
| 32 |
A topliss tree analysis of the HIV-protease inhibitory activity of 6-phenyl-4-hydroxy-pyran-2-ones |
TBA |
| 17 |
Structure-based drug design of nonpeptidic P2 substituents for HIV-1 protease inhibitors |
TBA |
| 9 |
Isophthalic acid derivatives: amino acid surrogates for the inhibition of HIV-1 protease |
TBA |
| 12 |
A systematic study of P1–P3 spanning sidechains for the inhibition of HIV-1 protease |
TBA |
| 29 |
2-Heterocyclic indole-3-sulfones as inhibitors of HIV-1 reverse transcriptase |
TBA |
| 14 |
Aminodiol HIV protease inhibitors. 2. 1,1-Dimethyl-2-hydroxyethyl carbamate derivatives with enhanced potency |
TBA |
| 4 |
A bis-[N-3-(1-hydroxy-1-methyl-ethyl)-benzyl)-cyclic urea as a HIV protease inhibitor |
TBA |
| 7 |
Ly316340: A potent HIV-1 protease inhibitor containing a high affinity octahydrothienopyridine hydroxyethylamine isostere |
TBA |
| 30 |
Evaluation of substituted benzamides as P2 ligands for symmetry-based inhibitors of HIV protease |
TBA |
| 15 |
Structure-based design of achiral anthranilamides as P2/P2′ surrogates for symmetry-based HIV protease inhibitors: design, synthesis, X-ray structure, enzyme inhibition and antiviral activity |
TBA |
| 13 |
Thiophene derivatives as extremely high affinity P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors |
TBA |
| 9 |
Substituted alkylpyridines as P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors: Improved pharmacokinetic profiles |
TBA |
| 10 |
Rational design of irreversible, pseudo-C2-symmetric hiv-1 protease inhibitors |
TBA |
| 23 |
α-hydroxyamide derived aminodiols as potent inhibitors of hiv protease |
TBA |
| 7 |
Symmetry-based HIV Protease inhibitors: rational design of 2-methylbenzamides as novel P2/P2′ ligands |
TBA |
| 14 |
Cyclic sulfone-3-carboxamides as novel P2-ligands for Ro 31-8959 based HIV-1 protease inhibitors |
TBA |
| 2 |
Synthesis of C2-symmetric inhibitors of the HIV-1 protease, with N,N′-substituted ethylenediamide and ethylenediamine linkers. |
TBA |
| 7 |
Design, structure activity and x-ray crystallographic studies of pseudosymmetrical nonpeptidyl HIV-1 protease inhibitors |
TBA |
| 7 |
Conformationally constrained HIV-1 protease inhibitors |
TBA |
| 13 |
Novel, extended transition state mimic in HIV-1 protease inhibitors with peripheral C-2-symmetry |
TBA |
| 13 |
Synthesis and evaluation of pyridyl analogs of L-735,524: Potent HIV-1 protease inhibitors |
TBA |
| 6 |
Carbocyclic analogues of hydroxyethylamine containing inhibitors of HIV proteinase |
TBA |
| 8 |
Non-peptide-based inhibitors of human immunodeficiency virus-1 protease |
TBA |
| 14 |
Beneficial replacement of the P1 phenylalanine side chain in HIV-1 protease inhibitors of the difluorostatone type |
TBA |
| 23 |
A new hydroxyethylamine class of HIV-1 protease inhibitors with high antiviral potency and oral bioavailability |
TBA |
| 19 |
Design, synthesis, and activity of conformationally-constrained macrocyclic peptide-based inhibitors of HIV protease |
TBA |
| 13 |
Novel conformationally constrained HIV-1 protease inhibitors: rational design, enzyme inhibition, and X-ray structure of an enzyme-inhibtor complex |
TBA |
| 14 |
D-amino acids as novel P2/P3 ligands for inhibitors of HIV-1 protease |
TBA |
| 7 |
New dipeptide isosteres useful for the inhibition of HIV-1 protease |
TBA |
| 1 |
Peptoid mimics of a C2-symmetric inhibitor of the HIV-1 protease. |
TBA |
| 4 |
De novo design of nonpeptidic HIV-1 protease inhibitors: Incorporation of structural water. |
TBA |
| 15 |
Increased antiviral activity of HIV protease inhibitors of the difluorostatone type bearing (R)-valinol derivatives as novel c-termini |
TBA |
| 8 |
Inhibition of human immunodeficiency virus-1 protease by a C2-symmetrical phosphinic acid amide |
TBA |
| 3 |
A concise enantioselective synthesis of rans-olefin dipeptide isosteres |
TBA |
| 16 |
Synthesis and biological evaluation of a series of HIV-1 protease inhibitors |
TBA |
| 17 |
Structure activity studies on pseudo-symmetrical HIV-1 protease inhibitors |
TBA |
| 5 |
The design and synthesis of novel hydroxyproline inhibitors of HIV-1 proteinase |
TBA |
| 22 |
Difunctional enols of N-protected amino acids as low molecular weight and novel inhibitors of HIV-1 protease. |
TBA |
| 10 |
Novel dimeric penicillin derived inhibitors of HIV-1 proteinase: interaction with the catalytic aspartates |
TBA |
| 17 |
Short and unexpectedly potent difluorostatone type inhibitors of HIV-1 protease |
TBA |
| 22 |
Novel pseudosymmetric inhibitors of HIV-1 protease |
TBA |
| 8 |
Nonpeptide HIV protease inhibitors designed to replace a bound water |
TBA |
17181152 |
17 |
Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization. |
The Scripps Research Institute |
16970402 |
8 |
HIV-1 protease mutations and inhibitor modifications monitored on a series of complexes. Structural basis for the effect of the A71V mutation on the active site. |
Academy of Sciences of The Czech Republic |
16854071 |
10 |
Molecular tongs containing amino acid mimetic fragments: new inhibitors of wild-type and mutated HIV-1 protease dimerization. |
Paris-Sud University |
16335934 |
10 |
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold. |
Uppsala University |
16203141 |
5 |
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
Abbott Laboratories |
15923115 |
6 |
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors. |
Peking University |
15893929 |
3 |
Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease. |
University of Debrecen |
15771440 |
3 |
Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
Tibotec |
15582426 |
3 |
New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties. |
University of The Mediterranean |
15566308 |
32 |
New constrained"molecular tongs" designed to dissociate HIV-1 protease dimer. |
Paris-Sud University |
15509178 |
37 |
Efficient evaluation of binding free energy using continuum electrostatics solvation. |
University of ZüRich |
15380231 |
2 |
Facile incorporation of urea pseudopeptides into protease substrate analogue inhibitors. |
Purdue University |
15225729 |
5 |
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors. |
Abbott Laboratories |
15149657 |
33 |
Novel nonpeptidic inhibitors of HIV-1 protease obtained via a new multicomponent chemistry strategy. |
Morphochem |
15139755 |
3 |
BREED: Generating novel inhibitors through hybridization of known ligands. Application to CDK2, p38, and HIV protease. |
Vertex Pharmaceuticals |
12852755 |
27 |
l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance. |
The University of Georgia |
12729673 |
39 |
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus. |
Merck Research Laboratories |
12699395 |
5 |
Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. |
Kyoto University |
12639540 |
10 |
Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors. |
Bristol-Myers Squibb |
12477350 |
47 |
Metal-dependent inhibition of HIV-1 integrase. |
University of Southern California |
12467624 |
9 |
Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere. |
Kyoto Pharmaceutical University |
12270162 |
4 |
Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'. |
Merck Research Laboratories |
12161148 |
17 |
Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains. |
Merck Research Laboratories |
12161147 |
5 |
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains. |
Merck Research Laboratories |
12109915 |
5 |
Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres. |
University of The Mediterranean |
11844665 |
38 |
A combinatorial library of indinavir analogues and its in vitro and in vivo studies. |
Merck Research Laboratories |
11784138 |
36 |
Elucidating the inhibiting mode of AHPBA derivatives against HIV-1 protease and building predictive 3D-QSAR models. |
Chinese Academy of Sciences |
32672965 |
44 |
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
University of Massachusetts Medical School |
32690263 |
29 |
Design and biological evaluation of novel HIV-1 protease inhibitors with isopropanol as P1' ligand to enhance binding with S1' subsite. |
Chinese Academy of Medical Science and Peking Union Medical College |
11378352 |
3 |
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir). |
Abbott Laboratories |
32551001 |
25 |
Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants. |
Chinese Academy of Medical Science and Peking Union Medical College |
32057582 |
29 |
Design, synthesis and biological evaluation of HIV-1 protease inhibitors with morpholine derivatives as P2 ligands in combination with cyclopropyl as P1' ligand. |
Jinzhou Medical University |
11206463 |
44 |
Design, synthesis, and biological evaluation of HIV/FIV protease inhibitors incorporating a conformationally constrained macrocycle with a small P3' residue. |
The Scripps Research Institute |
11128638 |
7 |
6-Hydroxy-1,3-dioxin-4-ones as non-peptidic HIV protease inhibitors. |
Institute of Science & Technology |
10987441 |
10 |
Use of proline bioisosteres in potential HIV protease inhibitors: phenylalanine-2-thiophenoxy-3-pyrrolidinone: synthesis and anti-HIV evaluation. |
Université |
10915042 |
3 |
Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library. |
Merck Research Laboratories |
10866387 |
1 |
'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker. |
Kyoto Pharmaceutical University |
10821715 |
34 |
A new class of HIV-1 integrase inhibitors: the 3,3,3', 3'-tetramethyl-1,1'-spirobi(indan)-5,5',6,6'-tetrol family. |
University of California |
10579836 |
7 |
Synthesis and biological evaluation of the first N-alkyl cage dimeric 4-aryl-1,4-dihydropyridines as novel nonpeptidic HIV-1 protease inhibitors. |
Martin-Luther-University Halle-Wittenberg |
10576691 |
11 |
Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents. |
Dupont Pharmaceuticals |
10514275 |
7 |
Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains. |
Uppsala University |
10465557 |
11 |
Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents. |
Dupont Pharmaceuticals |
10450973 |
21 |
4-hydroxy-5,6-dihydro-2H-pyran-2-ones.3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1' and S2' of the HIV-1 protease enzyme. |
Warner-Lambert |
10386921 |
33 |
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. |
Warner-Lambert |
10328309 |
3 |
Structure-based design of diaminopyranosides as a novel inhibitor core unit of HIV proteases. |
Biomolecular Engineering Research Institute |
10206539 |
1 |
A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor. |
Kyoto Pharmaceutical University |
10090778 |
9 |
Design, synthesis, and evaluation of conformationally constrained tongs, new inhibitors of HIV-1 protease dimerization. |
Université |
9934485 |
8 |
Design and synthesis of novel conformationally restricted HIV protease inhibitors. |
Vertex Pharmaceuticals |
9934484 |
32 |
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors. |
Vertex Pharmaceuticals |
9934481 |
9 |
Tricyclic ureas: a new class of HIV-1 protease inhibitors. |
Dupont Pharmaceuticals |
9934467 |
27 |
Unsymmetric nonpeptidic HIV protease inhibitors containing anthranilamide as a P2' ligand. |
Aids Drug Screening and Development Laboratory |
9925730 |
118 |
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis. |
Lindsley F. Kimball Research Institute |
9873554 |
3 |
NMR and topochemical studies of peptidomimetic HIV-I protease inhibitors containing a cis-epoxide amide isostere. |
Biotech Research Institute |
9873448 |
1 |
Synthesis and anti-HIV activities of symmetrical N1,N3-dibenzyl-2-hydroxy-propane derivatives. |
Université |
9871742 |
11 |
Non-peptidic HIV protease inhibitors: C2-symmetry-based design of bis-sulfonamide dihydropyrones. |
Pharmacia & Upjohn |
9871586 |
7 |
Endothiopeptide inhibitors of HIV-1 protease. |
Purdue University |
9871548 |
17 |
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues. |
Dupont Pharmaceuticals |
9871528 |
9 |
Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups. |
Dupont Pharmaceuticals |
9871514 |
16 |
Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand. |
Schering-Plough Research Institute |
9748353 |
13 |
Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors. Use of L-mannaric acid as a peptidomimetic scaffold. |
LinköPing University |
9632373 |
52 |
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues. |
Dupont Pharmaceuticals |
9622543 |
26 |
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency. |
Dupont Pharmaceuticals |
9572884 |
7 |
Cyclopropane-derived peptidomimetics. Design, synthesis, evaluation, and structure of novel HIV-1 protease inhibitors. |
National Cancer Institute-Frederick |
9484509 |
12 |
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy. |
Abbott Laboratories |
9406598 |
24 |
Nonsymmetrically substituted cyclic urea HIV protease inhibitors. |
Dupont Pharmaceuticals |
31188592 |
39 |
Why Some Targets Benefit from beyond Rule of Five Drugs. |
Boston University |
9003516 |
17 |
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV. |
Dupont Pharmaceuticals |
8917652 |
23 |
Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors. |
Pharmacia & Upjohn |
8863807 |
71 |
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis. |
Dupont Pharmaceuticals |
8831779 |
22 |
Cycloalkylpyranones and cycloalkyldihydropyrones as HIV protease inhibitors: exploring the impact of ring size on structure-activity relationships. |
Pharmacia and Upjohn |
8784440 |
3 |
New series of potent, orally bioavailable, non-peptidic cyclic sulfones as HIV-1 protease inhibitors. |
Gilead Sciences |
8709096 |
26 |
Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity. |
Universitá |
8676334 |
9 |
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents. |
University of North Carolina At Chapel Hill |
8632437 |
8 |
Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
Medichem Research |
8426362 |
46 |
Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol. |
Abbott Laboratories |
8360876 |
9 |
A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of gamma-turn mimetics into a model substrate. |
Smithkline Beecham Pharmaceuticals |
8230097 |
7 |
A series of penicillin-derived C2-symmetric inhibitors of HIV-1 proteinase: structural and modeling studies. |
Glaxo Group Research |
8164256 |
6 |
Calculation of relative differences in the binding free energies of HIV1 protease inhibitors: a thermodynamic cycle perturbation approach. |
Agouron Pharmaceuticals |
8126707 |
18 |
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases. |
University of California |
8057296 |
4 |
Structure-based design of HIV-1 protease inhibitors: replacement of two amides and a 10 pi-aromatic system by a fused bis-tetrahydrofuran. |
Merck Research Laboratories |
7966131 |
34 |
Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors: heterocyclic ring systems containing P1' and P2' substituents. |
Glaxo Research and Development |
7966128 |
2 |
Design, synthesis, and conformational analysis of a novel macrocyclic HIV-protease inhibitor. |
Marion Merrell Dow Research Institute |
7932573 |
19 |
L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor. |
Merck Research Laboratories |
7932533 |
11 |
Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere. |
Smithkline Beecham Pharmaceuticals |
7861404 |
29 |
Inhibitors of HIV-1 protease containing the novel and potent (R)-(hydroxyethyl)sulfonamide isostere. |
Searle Discovery Research |
7853337 |
12 |
Cosalane analogues with enhanced potencies as inhibitors of HIV-1 protease and integrase. |
Purdue University |
7830273 |
49 |
A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site. |
Merck Research Laboratories |
7650677 |
2 |
A check on rational drug design: crystal structure of a complex of human immunodeficiency virus type 1 protease with a novel gamma-turn mimetic inhibitor. |
Smithkline Beecham Pharmaceuticals |
7636862 |
8 |
Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores. |
Abbott Laboratories |
7543578 |
6 |
Anti-AIDS (acquired immune deficiency syndrome) agents. 17. New brominated hexahydroxybiphenyl derivatives as potent anti-HIV agents. |
University of North Carolina At Chapel Hill |
7540208 |
10 |
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
Tosoh |
7520080 |
18 |
Synthesis of naphthalenesulfonic acid small molecules as selective inhibitors of the DNA polymerase and ribonuclease H activities of HIV-1 reverse transcriptase. |
College of Pharmacy |
7473573 |
47 |
Structure-based design of nonpeptidic HIV protease inhibitors from a cyclooctylpyranone lead structure. |
Upjohn Laboratories |
11831910 |
60 |
Computational studies on tetrahydropyrimidine-2-one HIV-1 protease inhibitors: improving three-dimensional quantitative structure-activity relationship comparative molecular field analysis models by inclusion of calculated inhibitor- and receptor-based properties. |
University of Missouri-St. Louis |
12061879 |
44 |
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions. |
Harvard University |
2213822 |
12 |
Structure-based, C2 symmetric inhibitors of HIV protease. |
Abbott Laboratories |
2184237 |
17 |
Hydroxyethylamine analogues of the p17/p24 substrate cleavage site are tight-binding inhibitors of HIV protease. |
University of Wisconsin-Madison |
2002464 |
16 |
Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes. |
University of Wisconsin-Madison |
1635054 |
17 |
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity. |
Merck Research Laboratories |
1501235 |
11 |
Penicillin derived C2-symmetric dimers as novel inhibitors of HIV-1 proteinase. |
Glaxo Group Research |
15189032 |
66 |
Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs. |
Linkoping University |
9871543 |
17 |
Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases. |
Institut Curie |
15546737 |
59 |
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation. |
Avenida De La Industria |
15745832 |
35 |
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor. |
Wyeth-Ayerst Research |
11078204 |
19 |
Inhibitors of src tyrosine kinase: the preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines. |
Wyeth-Ayerst Research |