Journal of Medicinal Chemistry p. 4679 - 4686 (1995)
Update date:2022-08-04
Topics:
Dolle
Fan
Chi Hung Nguyen
Aubertin
Kirn
Andreola
Jamieson
Tarrago-Litvak
Bisagni
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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