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7-取代-4-羟基喹啉-3-羧酸的细胞呼吸抑制活性与范德华体积的关系

The relationship of cellular respiration inhibition activity of 7-substituted 4-hydroxyquinoline-3-carboxylic acids with van der Waals volume.

作者信息

Gupta S P, Bhatnagar R P, Singh P, Bindal M C

出版信息

Res Commun Chem Pathol Pharmacol. 1979 Jul;25(1):111-9.

PMID:451345
Abstract

The cellular respiratory inhibition activity of 7-substituted 4-hydroxyquinoline-3-carboxylic acids recently designed by Shah and Coats is found by regression analysis to be significantly correlated with van der Waals volume (V(w)). A parabolic correlation is obtained in case of ascites cell inhibition and a linear correlation in case of malate dehydrogenase inhibition. The correlation of both types of inhibition with a single parameter, V(w), makes the process of substituent selection in designing more potent inhibitors of whole respiratory cell much simpler.

摘要

沙阿和科茨最近设计的7-取代4-羟基喹啉-3-羧酸的细胞呼吸抑制活性,通过回归分析发现与范德华体积(V(w))显著相关。在腹水细胞抑制方面获得抛物线相关性,在苹果酸脱氢酶抑制方面获得线性相关性。两种抑制类型与单一参数V(w)的相关性,使得在设计更有效的全呼吸细胞抑制剂时的取代基选择过程变得简单得多。

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