一种合成新型钙依赖性脂肽抗生素马拉西丁A及其类似物的简洁策略。
A Concise Synthetic Strategy Towards the Novel Calcium-dependent Lipopeptide Antibiotic, Malacidin A and Analogues.
作者信息
Kovalenko Nadiia, Howard Georgina K, Swain Jonathan A, Hermant Yann, Cameron Alan J, Cook Gregory M, Ferguson Scott A, Stubbing Louise A, Harris Paul W R, Brimble Margaret A
机构信息
School of Chemical Sciences, The University of Auckland, Auckland, New Zealand.
School of Biological Sciences, The University of Auckland, Auckland, New Zealand.
出版信息
Front Chem. 2021 Aug 4;9:687875. doi: 10.3389/fchem.2021.687875. eCollection 2021.
Malacidin A is a novel calcium-dependent lipopeptide antibiotic with excellent activity against Gram-positive pathogens. Herein, a concise and robust synthetic route toward malacidin A is reported, employing 9-fluorenylmethoxycarbonyl solid-phase peptide synthesis of a linear precursor, including late-stage incorporation of the lipid tail, followed by solution-phase cyclization. The versatility of this synthetic strategy was further demonstrated by synthesis of a diastereomeric variant of malacidin A and a small library of simplified analogues with variation of the lipid moiety.
马拉西丁A是一种新型的钙依赖性脂肽抗生素，对革兰氏阳性病原体具有优异的活性。本文报道了一条简洁且可靠的合成马拉西丁A的路线，采用9-芴甲氧羰基固相肽合成线性前体，包括后期引入脂尾，随后进行溶液相环化。通过合成马拉西丁A的非对映异构体变体和一个具有脂部分变化的简化类似物小文库，进一步证明了这种合成策略的通用性。
Zotero 插件