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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Studies on novel bacterial translocase I inhibitors, A-500359s III. Deaminocaprolactam derivatives of capuramycin: A-500359 E,F,H,M-1 and M-2
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Studies on novel bacterial translocase I inhibitors, A-500359s III. Deaminocaprolactam derivatives of capuramycin: A-500359 E,F,H,M-1 and M-2

机译：新型细菌转运酶I抑制剂A-500359s III的研究。卡普拉霉素的脱氨基己内酰胺衍生物：A-500359 E，F，H，M-1和M-2

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摘要

Novel derivatives of capuramycin were obtained when 10 mM of 2-aminoethyl-L-cysteine (AEC), an inhibitor of aspartokinase, was added to the culture of Streptomyces griseus SANK 60196, the producer of A-500359. They were purified from the culture filtrate and their chemical structures were elucidated as a deminocaprolactam derivative of capuramycin designated as A-500359 F, A-500359 E, a methyl ester of A-500359 F, and A-500359 H, a 3'-demethyl derivative of A-500359 F. Two other compounds, A-500359 M-1 and A-500359 M-2, were purified from the same medium and their structures were elucidated. A-500359 E, F, H M-1 and M-2 inhibited bacterial translocase I with an IC_(50) of 0.027 muM, 1.1 muM, 0.008 muM, 0.058 muM and 0.010 muM, respectively. A-500359 E, M-1 and M-2 inhibited the growth of mycobacteria as well.
机译：将10 mM天冬氨酸激酶抑制剂的2-氨基乙基-L-半胱氨酸（AEC）添加到链霉菌SAN- 60196（A-500359的生产商）培养物中，即可获得新的卡普拉霉素衍生物。从培养滤液中纯化它们，并阐明其化学结构为卡普拉霉素的去甲己内酰胺衍生物，称为A-500359 F，A-500359 E，A-500359 F的甲酯和A-500359 H（3'-从同一培养基中纯化出另外两种化合物A-500359 M-1和A-500359 M-2，并阐明了它们的结构。 A-500359 E，F，HM-1和M-2抑制细菌转移酶I，IC_（50）分别为0.027μM，1.1μM，0.008μM，0.058μM和0.010μM。 A-500359 E，M-1和M-2也抑制分枝杆菌的生长。

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