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

DOI: 10.1021/jm00023a007

Source and publish data:

Journal of Medicinal Chemistry p. 4679 - 4686 (1995)

Update date:2022-08-04

Topics:

Authors:

Dolle Dolle

Fan Fan

Chi Hung Nguyen

Aubertin

Kirn Kirn

Andreola

Jamieson

Tarrago-Litvak

Bisagni Bisagni

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Article abstract of DOI:10.1021/jm00023a007

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.

Full text of DOI:10.1021/jm00023a007

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