题目: Tiacumicin Congeners with Improved Antibacterial Activity from a Halogenase-Inactivated Mutant

作者:Haibo Zhang, Xiaoxing Tian, Xiaohui Pu, Qingbo Zhang, Wenjun Zhang, and Changsheng Zhang*

刊物: Journal of Natural Products

年卷期页: 2018,81:1219-1224

摘要：Tiacumicin B (1, also known asfidaxomicin or difimicin) is a marketed drug for the treatment ofClostridium dif f icileinfections. The biosynthetic pathway of1has been studied inDactylosporangium aurantiacumsubsp.hamdenensisNRRL 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 thetiaM-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.