| Literature DB >> 7683054 |
J M Hoffman1, A M Smith, C S Rooney, T E Fisher, J S Wai, C M Thomas, D L Bamberger, J L Barnes, T M Williams, J H Jones.
Abstract
A new series of potent specific 2-pyridinone reverse transcriptase (RT) inhibitors was developed based on the preliminary development lead 3-[(phthalmido)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one (3), a non-nucleoside derivative which exhibited weak antiviral activity in cell culture against HIV-1 strain IIIB. One compound, 3-[(benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one (9,L-696,229), which was a highly selective antagonist of the RT enzyme (IC50 = 23 nM) and which inhibited the spread of HIV-1 IIIB infection by > 95% in MT4 human T-lymphoid cell culture (CIC95 = 50-100 nM), was selected for clinical evaluation as an antiviral agent.Entities:
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Year: 1993 PMID： 7683054 DOI： 10.1021/jm00060a002
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446