| Literature DB >> 9748354 |
R A Nugent1, S T Schlachter, M J Murphy, G J Cleek, T J Poel, D G Wishka, D R Graber, Y Yagi, B J Keiser, R A Olmsted, L A Kopta, S M Swaney, S M Poppe, J Morris, W G Tarpley, R C Thomas.
Abstract
A series of pyrimidine thioethers was synthesized and evaluated for inhibitory properties against wild-type HIV-1 reverse transcriptase (RT) and an RT carrying the resistance-conferring mutation P236L. Modifications of both the pyrimidine and the functionality attached through the thioether yielded several analogues, which demonstrated activity against both enzyme types, with IC50 values as low as 190 nM against wild-type and 66 nM against P236L RT. Evaluation of a select number of pyrimidine thioethers in cell culture showed that these compounds have excellent activity against HIV-1IIIB-WT and retain good activity against a laboratory-derived HIV-1MF delavirdine-resistant variant.Entities:
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Year: 1998 PMID： 9748354 DOI： 10.1021/jm9800806
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446