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. 1995 Nov 10;38(23):4679-86.
doi: 10.1021/jm00023a007.

A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors

V Dollé  1 , E Fan, C H Nguyen, A M Aubertin, A Kirn, M L Andreola, G Jamieson, L Tarrago-Litvak, E Bisagni
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A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors

V Dollé et al. J Med Chem. .

Abstract

4-(Arylthio)-pyridin-2(1H)-ones variously substituted in their 3-, 5-, and 6-positions have been synthesized as a new series of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)-pyridinone hybrid molecules. Biological studies revealed that some of them show potent HIV-1 specific reverse transcriptase inhibitory properties. Compounds 16 and 7c, the most active ones, inhibit the replication of HIV-1 at 3 and 6 nM, respectively.

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