Abstract
A new series of potent specific 2-pyridinone reverse transcriptase (RT) inhibitors was developed based on the preliminary development lead 3-[(phthalimido)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.
Original language | English |
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Pages (from-to) | 953-966 |
Number of pages | 14 |
Journal | Journal of Medicinal Chemistry |
Volume | 36 |
Issue number | 8 |
DOIs | |
State | Published - 1993 |