Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogs of 3-aminopyridin-2 (1H)-one

WS Saari, JS Wai, TE Fisher, CM Thomas…

Index: Saari, Walfred S.; Wai, John S.; Fisher, Thorsten E.; Thomas, Craig M.; Hoffman, Jacob M.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 21 p. 3792 - 3802

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Citation Number: 103

Abstract

A series of nonnucleoside 3-aminopyridin-2 (lH)-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 IC60 values as low as 19 nM in the enzyme assay using rC* dG as templateprimer. Two compounds from this aeries, 3-[[(4, 7-dimethylbenoxazol-2- yl) methyl]-aminol-5-ethyl-6-methylpyridin-2 (lH)-one (34, L-697,639) and the ...