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

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

  • J Med Chem. 1995 Nov 10;38(23):4679-86. doi: 10.1021/jm00023a007.
V Dollé 1,  E Fan,  C H Nguyen,  A M Aubertin,  A Kirn,  M L Andreola,  G Jamieson,  L Tarrago-Litvak,  E Bisagni
Affiliations

Affiliation

  • 1 URA 1387 CNRS, Synthèse Organique, Institut Curie, Section de Recherche, Orsay, France.
PMID: 7473595 DOI: 10.1021/jm00023a007
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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