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[N4-取代磺胺类药物的分子结构与抗菌活性之间的关系]

[Relation between molecular structure and the antibacterial activity of N4-substituted sulfanilamides].

作者信息

Vŭrbanova S, Danailov D, Kolev K K, Stefanov V

出版信息

Vet Med Nauki. 1987;24(10):67-70.

PMID:3450084
Abstract

With the aim of establishing a correlation between chemical structure and biologic activity of series N, N'-replaced carbamide and thiocarbamide derivatives, containing sulfanilamide group their antibacterial activity has been studied. The microbiologic screening towards eight kinds of gram-positive and gram-negative microorganisms showed that the substitutes in N and N' in the carbamide or thiocarbamide structure influence the force of the effect as well as the kind of microorganisms in which that effect is exhibited. Ascertained was that together with the increase of the number of carbon atoms is strengthen the antibacterial activity (highest in C4) as the derivatives containing aryl radical show higher activity than those containing alkyl radical. The bringing of halogenic atoms in the molecule of the synthesized derivatives increases considerably the antibacterial activity which is expressed mainly in the combinations containing Cl-atom in m-position of the benzene nucleus.

摘要

为了建立含磺胺基团的N,N'-取代脲和硫脲衍生物系列的化学结构与生物活性之间的相关性,对它们的抗菌活性进行了研究。针对八种革兰氏阳性和革兰氏阴性微生物的微生物筛选表明,脲或硫脲结构中N和N'的取代基会影响作用强度以及表现出该作用的微生物种类。已确定随着碳原子数的增加,抗菌活性增强(在C4时最高),因为含芳基的衍生物比含烷基的衍生物表现出更高的活性。在合成衍生物的分子中引入卤原子会大大增加抗菌活性,这主要表现在苯核间位含Cl原子的组合中。

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