QUATERNARY AMMONIUM-SALTS .45. QUANTITATIVE RELATIONSHIPS BETWEEN STRUCTURE AND ANTIMICROBIAL ACTIVITY OF NEW SOFT BISQUATERNARY AMMONIUM-SALTS
QUATERNARY AMMONIUM-SALTS .45. QUANTITATIVE RELATIONSHIPS BETWEEN STRUCTURE AND ANTIMICROBIAL ACTIVITY OF NEW SOFT BISQUATERNARY AMMONIUM-SALTS
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DOI：
10.1007/bf02814644
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发表时间：
1994-01-01
影响因子：
2.6
通讯作者：
MLYNARCIK, D
中科院分区：
文献类型：
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作者：
PAVLIKOVAMORICKA, M;LACKO, I;MLYNARCIK, D
由戊二酸双-(2-二甲氨基乙基)酯衍生的新型表面活性双季铵盐对革兰氏阳性菌、革兰氏阴性菌和酵母菌具有高效的杀灭作用。通过定量结构-活性方法学验证了结构、亲脂性和抑菌效果之间的关系。用Kubinyi的双线性模型描述了生物活性与结构和亲脂性(用临界胶束浓度-CMC表示)的非线性依赖关系。最有效的化合物是11-12个碳原子烷基链的化合物，其cmc值在0.7-1.0 mmol/L左右，这些衍生物具有较高的抗菌活性，特别是对革兰氏阴性菌。
New surface-active bisquaternary ammonium salts derived from bis-(2-dimethylaminoethyl) ester of glutaric acid are highly effective against representatives of Gram-positive, Gram-negative bacteria and yeasts. Relationships between structure, lipophilicity and antimicrobial effectiveness were demonstrated by quantitative structure-activity methodology. The nonlinear dependence of biological activity on the structure as well as lipophilicity (expressed as critical micelle concentration - CMC) was shown using Kubinyi's bilinear model. The most effective compounds were those with the alkyl chain of 11-12 carbon atoms and with the CMC values around 0.7-1.0 mmol/L. These derivatives possessed higher antimicrobial activity particularly to Gram-negative bacteria.