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烷氧基取代苯基氨基甲酸哌啶基乙酯季铵盐抗分枝杆菌活性的定量构效关系研究

QSAR study of antimycobacterial activity of quaternary ammonium salts of piperidinylethyl esters of alkoxysubstituted phenylcarbamic acids.

作者信息

Waisser K, Dolezal R, Palát K, Cizmárik J, Kaustová J

机构信息

Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Králové, Czechia.

出版信息

Folia Microbiol (Praha). 2006;51(1):21-4. doi: 10.1007/BF02931444.

Abstract

A series of 17 halogenides of quaternary ammonium salts of the alkylpiperidinylethyl esters of 2-pentoxy (and 2-heptoxy) substituted phenylcarbamic acids were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, M. kansasii, and M. avium. Correlation of this action with lipophilicity (log P, 1-octanol-water system) was used for the description of the structure-antimycobacterial activity relationships (QSARs). The activity increased with the increasing lipophilicity of the compounds.

摘要

对一系列17种2-戊氧基(和2-庚氧基)取代苯基氨基甲酸烷基哌啶基乙酯的季铵盐卤化物进行了体外抗结核分枝杆菌、堪萨斯分枝杆菌和鸟分枝杆菌活性评估。利用这种作用与亲脂性(log P,1-辛醇-水体系)的相关性来描述结构-抗分枝杆菌活性关系(QSARs)。活性随着化合物亲脂性的增加而增强。

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