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

被引：104

作者：

DOLLE, V

FAN, E

NGUYEN, CH

AUBERTIN, AM

KIRN, A

ANDREOLA, ML

JAMIESON, G

TARRAGOLITVAK, L

BISAGNI, E

机构：

[1] INST VIROL,INSERM,U74,F-67000 STRASBOURG,FRANCE

[2] INST BIOCHIM & GENET CELLULAIRES,REPLICAT & EXPRESS GENOMES EUCARYOTES & RETROVIRA,F-33077 BORDEAUX,FRANCE

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 38卷 / 23期

关键词：

D O I：

10.1021/jm00023a007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：4679 / 4686

页数：8

共 24 条

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