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[哌啶的一系列N-芳基丁烯基衍生物的结构与生物活性之间的关系]

[Relationship between the structure and biological activity of a series of N-arylbutenyl derivatives of piperidine].

作者信息

Pis'ko G T, Buriak V S, Ganushchak N I

出版信息

Farmakol Toksikol. 1977 Mar-Apr;40(2):210-5.

PMID:856629
Abstract

A total of 74 compounds were synthetized and their biological activity studied on 3888 animals and on 347 strains of various microorganisms and fungi. The drugs have a moderate toxicity. The compounds containing an ester grouping of the alkyl radical with an odd number of carbon atoms are less toxic than are those with their even number. Most toxic are drugs that carry a chlorine atom in the orthoposition of the benzene nucleus and are less so the ones containing the bromine atom in this position. The toxicity of bis-quaternary salts diminishes with the rising molecular weight of the radical, this not being found to happen in the series of monoquaternary compounds. Most drugs display a locally anesthetizing and marked antimicrobial and antifungal properties. The antimicrobial activity appears with R-CH3, gradually increasing and becoming maximal with R-C10H21.

摘要

共合成了74种化合物,并在3888只动物以及347株各种微生物和真菌上研究了它们的生物活性。这些药物具有中等毒性。含有奇数个碳原子的烷基酯基团的化合物比含有偶数个碳原子的化合物毒性小。毒性最大的是在苯环邻位带有氯原子的药物,而在该位置含有溴原子的药物毒性较小。双季铵盐的毒性随着基团分子量的增加而降低,而在单季铵化合物系列中未发现这种情况。大多数药物具有局部麻醉以及显著的抗菌和抗真菌特性。抗菌活性在R-CH₃时出现,随着R-C₁₀H₂₁逐渐增加并达到最大值。

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