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

Veterinarno-meditsinski nauki Pub Date : 1987-01-01
S Vŭrbanova, D Danailov, K K Kolev, V Stefanov
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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.

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[分子结构与n4取代磺胺类抗菌活性的关系]。
为了建立N系列、N′取代氨基脲和含磺胺基硫代氨基脲衍生物的化学结构与生物活性之间的关系,研究了它们的抗菌活性。对8种革兰氏阳性和革兰氏阴性微生物的微生物学筛选表明,尿素或硫脲结构中N和N'的取代物影响了效应的强度,也影响了产生效应的微生物种类。结果表明,随着碳原子数的增加,含芳基自由基的衍生物比含烷基自由基的衍生物具有更高的抑菌活性(以C4为最高)。在合成的衍生物分子中引入卤素原子后,其抑菌活性显著提高,这主要表现在苯核m位含有cl原子的组合中。
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