Design, synthesis and antiviral activity of new pyridinone derivatives

被引:6
|
作者
Jourdan, F
Renault, J
Fossey, C
Bureau, R
Laduree, D
Robba, M
Aubertin, AM
Kirn, A
机构
[1] CERMN,F-14032 CAEN,FRANCE
[2] INSERM U74,F-67000 STRASBOURG,FRANCE
来源
ANTIVIRAL CHEMISTRY & CHEMOTHERAPY | 1997年 / 8卷 / 02期
关键词
3-[(arylmethyl)oxy-methyl]pyridin-2-ones; HIV-1; EBPU; L-696,229; reverse transcriptase;
D O I
10.1177/095632029700800210
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A molecular modelling study was carried out in order to compare the structural and electronic properties of the pyridinone L-696,229 and the HEPT derivative EBPU. This comparison led to a hybrid structure, 3-(benzyloxymethyl)-5-ethyl-6-methylpyridin-2-one [18a], which revealed a good structural correlation with the models. A series of 2-[(arylmethyl)oxymethyl]pyridin-2-ones related to [18a] was synthesized and tested for antiviral activity against human immunodeficiency virus type 1 (HIV-1). Compound [18a] and four other derivatives showed anti-HIV-1 activity.
引用
收藏
页码:161 / 172
页数:12
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