Quantitative structure-activity relationship studies on anti-HIV-1 TIBO derivatives as inhibitors of viral reverse transcriptase

被引：18

作者：

Gupta, SP

Garg, R

机构：

[1] Department of Chemistry, Birla Inst. of Technol. and Science

来源：

JOURNAL OF ENZYME INHIBITION | 1996年 / 11卷 / 01期

关键词：

quantitative structure-activity relationship; HIV-1 reverse transcriptase inhibitors; TIBO derivatives; QSAR;

D O I：

10.3109/14756369609038219

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：

The anti-human-immunodeficiency-virus (HIV-1) activity of the derivatives of 4,5,6,7-tetrahydro-5-methylimidazo [4,5,1-jk] [1,4] benzodiazepin-2(1H)-one (TIBO) that have been found to elicit their action through the allosteric inhibition of the enzyme viral reverse transcriptase (VRT) is analysed in relation to the physicochemical properties of the molecules. Significant correlations are obtained between the activity and the hydrophobic constant and some dummy parameters of substituents. Based on these findings, the mechanism of action of these anti-HIV drugs is discussed.

引用

收藏

页码：23 / 32

页数：10

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