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

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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@article{Doll1995ANS, title={A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors.}, author={Val{\'e}rie Doll{\'e} and Erkang Fan and Chi Hung Nguyen and A. M. Aubertin and Anette Kirn and M L Andr{\'e}ola and Gordon A. Jamieson and Laura Tarrago-Litvak and Emile Bisagni}, journal={Journal of medicinal chemistry}, year={1995}, volume={38 23}, pages={4679-86} }