A NEW SERIES OF PYRIDINONE DERIVATIVES AS POTENT NONNUCLEOSIDE HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 SPECIFIC REVERSE-TRANSCRIPTASE INHIBITORS

Authors
DOLLE V FAN E NGUYEN CH AUBERTIN AM KIRN A ANDREOLA ML JAMIESON G TARRAGOLITVAK L BISAGNI E
Citation
V. Dolle et al., A NEW SERIES OF PYRIDINONE DERIVATIVES AS POTENT NONNUCLEOSIDE HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 SPECIFIC REVERSE-TRANSCRIPTASE INHIBITORS, Journal of medicinal chemistry, 38(23), 1995, pp. 4679-4686
Citations number
24
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
38
Issue
23
Year of publication
1995
Pages
4679 - 4686
Database
ISI
SICI code
0022-2623(1995)38:23<4679:ANSOPD>2.0.ZU;2-X
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-hydrox yethoxy)methyl]-6-(phenylthio)thymine (HEPT)-pyridinone hybrid molecul es. Biological studies revealed that some of them show potent HIV-1 sp ecific reverse transcriptase inhibitory properties. Compounds 16 and 7 c, the most active ones, inhibit the replication of HIV-1 at 3 and 6 n M, respectively.