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来自链霉菌 I08A 1776 的三种新的 12-氨基甲酰基链丝菌素。

Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.

机构信息

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.

出版信息

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6151-4. doi: 10.1016/j.bmcl.2012.08.003. Epub 2012 Aug 10.

Abstract

Two new streptothricins (1 and 2) and a new streptothricin acid derivative (3), all with the carbamoyl group substituted at C-12 of the gulosamine moiety, together with the known N(β)-acetylstreptothricin D acid (4), have been isolated from the culture broth of Streptomyces sp. I08A 1776. The structures of the new compounds were determined by MS, CD, and 1D and 2D NMR spectroscopic data analysis. The isolated compounds were evaluated for antibacterial and antifungal activities. Streptothricin E (6) showed potent activity against the clinically isolated extensively drug-resistant Mycobacterium tuberculosis with MIC values of 0.25-0.5μg/mL.

摘要

从链霉菌 sp. I08A 1776 的发酵液中分离得到了两个新的链霉菌素(1 和 2)和一个新的链霉菌素酸衍生物(3),它们都在葡糖胺部分的 C-12 位上取代了氨基甲酰基,以及已知的 N(β)-乙酰链霉菌素 D 酸(4)。新化合物的结构通过 MS、CD 和 1D 和 2D NMR 光谱数据分析确定。对分离得到的化合物进行了抗菌和抗真菌活性评价。链霉菌素 E(6)对临床分离的广泛耐药结核分枝杆菌具有很强的活性,MIC 值为 0.25-0.5μg/mL。

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