Tiacumicin Congeners with Improved Antibacterial Activity from a Halogenase-Inactivated Mutant,Journal of Natural Products

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Tiacumicin Congeners with Improved Antibacterial Activity from a Halogenase-Inactivated Mutant
Journal of Natural Products ( IF 3.3 ) Pub Date : 2018-04-20 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00990
Haibo Zhang ₁ , Xiaoxing Tian ₂ , Xiaohui Pu ₂ , Qingbo Zhang ₁ , Wenjun Zhang ₁ , Changsheng Zhang ₁

Affiliation

Tiacumicin B (1, also known as fidaxomicin or difimicin) is a marketed drug for the treatment of Clostridium difficile infections. The biosynthetic pathway of 1 has been studied in Dactylosporangium aurantiacum subsp. hamdenensis NRRL 18085 and has enabled the identification of TiaM as a tailoring dihalogenase. Herein we report the isolation, structure elucidation, and bioactivity evaluation of 14 tiacumicin congeners (including 11 new ones) from the tiaM-inactivated mutant. A new tiacumicin congener, 3, with a propyl group at C-7‴ of the aromatic ring was found to exhibit improved antibacterial activity.

中文翻译：

Tiacumicin同源物，具有卤素酶灭活突变体改善的抗菌活性。

Tiacumicin B（Tiacumicin B ，替卡米星B ，Tiacumicin B ，Tiacumicin B）（1，也称为非达索霉素（fidaxomicin，difimicin））是一种用于治疗艰难梭菌感染的市售药物。的生物合成途径1进行了研究孢囊橙黄亚种。hamdenensis NRRL 18085，并已将TiaM鉴定为特制的二卤化酶。在此，我们报告了从tiaM失活突变体中分离出的14种tiacumicin同系物（包括11个新的同系物）的分离，结构解析和生物活性评估。发现一种新的头孢菌素同源物3在芳香环的C-7′处带有一个丙基，具有更好的抗菌活性。

更新日期：2018-04-20

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