Sanofi Research & Development, TSU Infectious Disease, 195, route d'Espagne BP 13669 31036 Toulouse Cedex 1, France.
Bioorg Med Chem Lett. 2012 Oct 1;22(19):6292-6. doi: 10.1016/j.bmcl.2012.06.107. Epub 2012 Jul 9.
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.
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。