Inhibition of HIV-1 capsid assembly: Optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol- 1-yl)-1H-benzimidazole scaffold

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 24, 2012, Pages 7512-7517

  Tremblay, Martin ^a   Bonneau, Pierre ^a   Bousquet, Yves ^a   Deroy, Patrick ^a   Duan, Jianmin ^a   Duplessis, Martin ^a   Gagnon, Alexandre ^b   Garneau, Michel ^a   Goudreau, Nathalie ^a   Guse, Ingrid ^a   Hucke, Oliver ^a   Kawai, Stephen H ^a   Lemke, Christopher T ^a   Mason, Stephen W ^c   Simoneau, Bruno ^a   Surprenant, Simon ^a   Titolo, Steve ^a   Yoakim, Christiane ^a  

^a BOEHRINGER INGELHEIM CANADA LTD   (Canada)

^b UNIVERSITÉ DU QUÉBEC À MONTRÉAL   (Canada)

^c BRISTOL MYERS SQUIBB   (United States)

Author keywords

Benzimidazole; Capsid assembly inhibitor; HIV 1; X ray crystal structure

Indexed keywords

5 (5 FURAN 2 YL PYRAZOL 1 YL) 1H BENZIMIDAZOLE; ANTIVIRUS AGENT; BENZIMIDAZOLE; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ANTIVIRAL ACTIVITY; ARTICLE; COMPLEX FORMATION; CYTOTOXICITY; HUMAN IMMUNODEFICIENCY VIRUS 1; IC 50; NONHUMAN; PROTEIN INTERACTION; STRUCTURE ACTIVITY RELATION; VIRUS ASSEMBLY; VIRUS CAPSID; X RAY;

ANTIVIRAL AGENTS; BENZIMIDAZOLES; CAPSID PROTEINS; DOSE-RESPONSE RELATIONSHIP, DRUG; HIV-1; MICROBIAL SENSITIVITY TESTS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP;

HUMAN IMMUNODEFICIENCY VIRUS 1; MIRIDAE;

EID: 84870249453     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.10.034     Document Type: Article

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