| Literature DB >> 12161148 |
Joseph L Duffy1, Nancy J Kevin, Brian A Kirk, Kevin T Chapman, William A Schleif, David B Olsen, Mark Stahlhut, Carrie A Rutkowski, Lawrence C Kuo, Lixia Jin, Jiunn H Lin, Emilio A Emini, James R Tata.
Abstract
Substitution of the t-butylcarboxamide substituent in analogues of the HIV protease inhibitor (PI) Indinavir with a trifluoroethylamide moiety confers greater potency against both the wild-type (NL4-3) virus and PI-resistant HIV. The trifluoroethyl substituent also affords a slower clearance rate in vivo (dogs); however, this may be due to more potent inhibition of at least two P450 isoforms.Entities:
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Year: 2002 PMID： 12161148 DOI： 10.1016/s0960-894x(02)00425-0
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823