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Chemistry and Biology of the Clinically Used Macrolactone Antibiotic Fidaxomicin
Helvetica Chimica Acta ( IF 1.8 ) Pub Date : 2020-04-09 , DOI: 10.1002/hlca.202000038
Andrea Dorst 1 , Karl Gademann 1
Affiliation  

Fidaxomicin (1, lipiarmycin A3, clostomicin B1, tiacumicin B) constitutes a glycosylated 18‐membered macrolactone and is a natural product isolated from various soil bacteria. Since 2011, fidaxomicin is a marketed antibiotic for the treatment of intestine infections caused by C. difficile in the clinic. Its promising in vitro antibacterial properties against resistant S. aureus and M. tuberculosis continue to attract interest. This review article describes the early history of the antibiotic fidaxomicin and highlights recent advances in the field, such as the elucidation of its mode of action and biosynthesis, as well as known derivatives. Furthermore, different synthetic strategies towards the total synthesis of fidaxomicin are summarized.

中文翻译:

临床上使用的大内酯类抗生素非达米星的化学和生物学

非达索霉素(1,利比霉素A3,clostomicin B1,tiacumicin B)构成糖基化的18元巨内酯,是从各种土壤细菌中分离出来的天然产物。自2011年以来,非达索霉素是市售的抗生素,用于治疗临床上由艰难梭菌引起的肠道感染。它具有抗金黄色葡萄球菌结核分枝杆菌的体外抗菌特性继续引起人们的兴趣。这篇综述文章描述了抗生素非达索霉素的早期历史,并重点介绍了该领域的最新进展,例如阐明了其作用方式和生物合成以及已知的衍生物。此外,总结了针对全合成非达索霉素的不同合成策略。
更新日期:2020-04-09
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