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亚美尼亚螺菌素,一类新型的抗菌药物:5-氯-亚美尼亚螺菌素 A 的抗菌活性和全合成。

Armeniaspiroles, a new class of antibacterials: Antibacterial activities and total synthesis of 5-chloro-Armeniaspirole A.

机构信息

Sanofi Research & Development, TSU Infectious Disease, 195, route d'Espagne BP 13669 31036 Toulouse Cedex 1, France.

出版信息

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6292-6. doi: 10.1016/j.bmcl.2012.06.107. Epub 2012 Jul 9.

Abstract

Armeniaspiroles, a novel class of natural products isolated from Streptomyces armeniacus, are characterized by a novel spiro[4.4]non-8-ene scaffold. Various derivatives of Armeniaspiroles could be obtained by halogenation, alkylation, addition/elimination or reductions. A total synthesis of the 5-chloro analog of Armeniaspirole A has been accomplished in a linear six-step sequence. 5-Chloro-Armeniaspirole A exhibits good activity against a range of multidrug-resistant, Gram-positive bacterial pathogens.

摘要

从链霉菌属(Streptomyces armeniacus)中分离得到的Armeniaspiroles 是一类新型天然产物,其特征在于具有新型的螺[4.4]壬-8-烯骨架。通过卤化、烷基化、加成/消除或还原等反应可以得到各种 Armeniaspiroles 的衍生物。已经通过六步线性序列完成了 5-氯-Armeniaspirole A 的全合成。5-氯-Armeniaspirole A 对多种多药耐药、革兰氏阳性细菌病原体具有良好的活性。

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