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Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 1985-12-01 , DOI: 10.1021/jm00150a006
R Okachi , H Niino , K Kitaura , K Mineura , Y Nakamizo , Y Murayama , T Ono , A Nakamizo

A series of compounds, which are analogues of 2,2'-dithiobis(benzamide), were synthesized and tested for in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv including resistant strains against streptomycin, kanamycin, or isonicotinic acid hydrazide. MICs of these compounds against atypical mycobacteria, Mycobacterium kansasii and Mycobacterium intracellulare were also examined. Structure-activity relationships were found in a series of (acyloxy)alkyl ester derivatives depending upon the length of alkyl carbon chain. The MIC of the most potent compound, 2,2'-dithiobis[N-[3-(decanoyloxy)propyl]benzamide] [56] was superior or at least equivalent to streptomycin, kanamycin, and ethanbutol. All the compounds showed no cross-resistance between the current antitubercular agents.

中文翻译:

2,2'-二硫代双(苯甲酰胺)衍生物的合成及其对分枝杆菌种类的抗菌活性。

合成了2,2'-二硫代双(苯甲酰胺)类似物的一系列化合物,并测试了其对结核分枝杆菌H37Rv的体外抗菌活性,包括对链霉素,卡那霉素或异烟酸酰肼的抗性菌株。还检查了这些化合物对非典型分枝杆菌,堪萨斯分枝杆菌和胞内分枝杆菌的MIC。在一系列(酰氧基)烷基酯衍生物中发现了结构-活性关系,这取决于烷基碳链的长度。最有效的化合物2,2'-二硫代双[N- [3-(癸酰氧基)丙基]苯甲酰胺] [56]的MIC优于或至少等同于链霉素,卡那霉素和乙胺丁醇。在目前的抗结核药之间,所有化合物均无交叉抗性。
更新日期:2019-11-01
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