选定的吩噻嗪类和噻吩蒽类对生长缓慢的分枝杆菌的抑菌效果。

J E Kristiansen, B Vergmann
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引用次数: 55

摘要

本研究的目的是阐明各种吩噻嗪和噻吩蒽衍生物对分枝杆菌的体外抑菌作用。通过对分枝杆菌菌株生长的抑制作用,表明氯戊噻醇的抑制作用约为氯丙嗪(CPZ)的两倍,左旋丙嗪-马来酸盐的抑制作用约为CPZ的一半。用同样的方法测量,氟苯硫醇的立体异构体化合物比氯苯硫醇和氯原硫森的立体异构体化合物更有效。这两种最后命名的化合物效力相等。噻吩衍生物的立体异构体类似物对生长缓慢的分枝杆菌具有相同的抗菌效力。所调查的分枝杆菌菌株在顺式(Z)-和反式(E)-硫代蒽化合物之间的敏感性没有差异。除了结核分枝杆菌外,耐药程度更高的分枝杆菌,如鸟分枝杆菌和胞内分枝杆菌,在所调查的浓度范围内也很敏感,这似乎特别有希望。综上所述,这些结果可能会刺激研究硫代蒽类在体内的抗菌作用。
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The antibacterial effect of selected phenothiazines and thioxanthenes on slow-growing mycobacteria.

The aim of the present investigation was to illustrate the antibacterial effect of various phenothiazine and thioxanthene derivatives on mycobacteria in vitro. It was demonstrated that clopenthixol is about twice as potent as chlorpromazine (CPZ) and levomepromazine-maleate is about half as potent as CPZ, measured by the inhibitory effect on the growth of the mycobacterial strains. Measured in the same way the stereoisomeric compounds of flupenthixol are shown to be more potent than the stereo-isomeric compounds of clopenthixol and chlorprothixen. The two last-named compounds are equal in potency. The stereo-isomeric analogs of the thioxanthene derivatives are equal in antibacterial potency against the slow-growing mycobacteria. The mycobacterial strains investigated show no difference in sensitivity between the cis (Z)--and and trans (E)--compounds of the thioxanthenes. It seems particularly promising that also the more resistant mycobacteria other than Mycobacterium tuberculosis, e.g. M. avium and M. intracellulare, are sensitive in the concentration range investigated. Considered as a whole, these results might be a stimulus to investigate the antimicrobial effect of the thioxanthenes in vivo.

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