Journal of Medicinal Chemistry p. 3792 - 3802 (1992)
Update date:2022-07-31
Topics:
Saari, Walfred S.
Wai, John S.
Fisher, Thorsten E.
Thomas, Craig M.
Hoffman, Jacob M.
et al.
A series of nonnulceoside 3-aminopyridin-2(1H)-one derivatives was synthesized and evaluated for HIV-1 RT inhibitory properties.Several analogs proved to be potent and highly selective antagonists with in vitro IC50 values as low as 19 nM in the enzyme assay using rC*dG as template*primer.Two compounds from this series, 3-<<4,7-dimethylbenzoxazol-2-yl)methyl>amino>-5-ethyl-6-methylpyridin-2(1H)-one (34, L-697,639) and the corresponding 4,7-dichloro analogue (37, L-697,661) inhibited the spread of HIV-1 IIIb infection by 95percent in MT4 cell culture at concentrations of 25-50 nM and were selected for clinical trials as antiviral agents.
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