Bis tertiary amide inhibitors of the HIV-1 protease generated via protein structure-based iterative design

Journal of Medicinal Chemistry

Volumn 39, Issue 14, 1996, Pages 2795-2811

  Melnick, Michael ^a   Reich, Siegfried H ^a   Lewis, Kathy K ^a   Mitchell Jr , Lennert J ^a   Nguyen, Dzuy ^a   Trippe, Anthony J ^a   Dawson, Heather ^a   Davies II, Jay F ^a   Appelt, Krzysztof ^a   Wu, Bor Wen ^a   Musick, Linda ^a   Gehlhaar, Dan K ^a   Webber, Stephanie ^a   Shetty, Bhasker ^a   Kosa, Maha ^a   Kahil, Deborah ^a   Andrada, Dominic ^a  

^a AGOURON PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AG 1132; AMIDE; ENZYME INHIBITOR; N TERT BUTYL 2 [2 HYDROXY 4 PHENYL 3 [[N (2 QUINOLYLCARBONYL)ASPARAGINYL]AMINO]BUTYL]BENZAMIDE; PROTEINASE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BINDING KINETICS; CELL CULTURE; CRYSTALLOGRAPHY; ENZYME ACTIVITY; ENZYME INHIBITION; LIGAND BINDING; PROTEIN STRUCTURE;

AMIDES; ANIMALS; ANTIVIRAL AGENTS; CELL LINE; DOGS; DRUG DESIGN; HAPLORHINI; HIV PROTEASE INHIBITORS; HIV-1; HUMANS; MICE; MOLECULAR STRUCTURE; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 8944241764     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm960092w     Document Type: Article

References (32)

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14. Previous paper: Reich, S. H.; Melnick, M.; Pino, M. J.; Fuhry, M. A. M.; Trippe, A. J.; Appelt, K.; Davies, J. F.; Wu, B.-W.; Musick, L. Structure-Based Design and Synthesis of Substituted 2-Butanols as Nonpeptidic Inhibitors of HIV Protease: Secondary Amide Series. J. Med. Chem. 1996, 39, 2781-2794.
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28. Prepared by the same method used to prepare 10d, see previous reference.
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32. Prepared unambiguously from 5-amino-2-methylbenzoic acid; CAS Registry No. 7499-06-1.