| Literature DB >> 15537347 |
George A Freeman1, C Webster Andrews Iii, Andrew L Hopkins, Gina S Lowell, Lee T Schaller, Jill R Cowan, Stephen S Gonzales, George W Koszalka, Richard J Hazen, Lawrence R Boone, Rob G Ferris, Katrina L Creech, Grace B Roberts, Steven A Short, Kurt Weaver, David J Reynolds, John Milton, Jingshan Ren, David I Stuart, David K Stammers, Joseph H Chan.
Abstract
HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) are part of the combination therapy currently used to treat HIV infection. The features of a new NNRTI drug for HIV treatment must include selective potent activity against both wild-type virus as well as against mutant virus that have been selected by use of current antiretroviral treatment regimens. Based on analogy with known HIV-1 NNRTI inhibitors and modeling studies utilizing the X-ray crystal structure of inhibitors bound in the HIV-1 RT, a series of substituted 2-quinolones was synthesized and evaluated as HIV-1 inhibitors.Entities:
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Year: 2004 PMID： 15537347 DOI： 10.1021/jm040072r
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446