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Published on: January 26, 2016
Diversity-oriented routes to thiopeptide antibiotics: total synthesis and biological evaluation of micrococcin P2
Hee-Jong Hwang1,2, Young-Jin Son1,3, Dahyun Kim1
1A&J Science Co., Ltd, 80 Chumbok Ro, Dong Gu, Daegu, 41061, Republic of Korea. hwanghj@anjscience.co.kr.
Abstract:
We report the first total synthesis of micrococcin P2 (MP2, 1) by a diversity-oriented route that incorporates a number of refinements relative to earlier syntheses. Biological data regarding the activity of 1 against a range of human pathogens are also provided. Furthermore, we disclose a chemical property of MP2 that greatly facilitates medicinal chemistry work in the micrococcin area and describe a method to obtain MP2 by fermentation in B. subtilis.
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