New pleuromutilin derivatives with enhanced antimicrobial activity. I. Synthesis.
作者:HELMUT EGGER、HELLMUTH REINSHAGEN
DOI:10.7164/antibiotics.29.915
日期:——
A series of new derivatives of the antibiotic pleuromutilin, produced by some Basidiomycetes, was synthesized by chemical modification of natural pleuromutilin. Most of them contain basic functional groups in the side chain at C14 of the mutilin skeleton. The monotosylate of pleuromutilin was used as a versatile intermediate for displacement by N-, O- and S-nucleophiles.
一些担子菌所产生的一系列的抗生素截短菌素的新的衍生物,通过对天然截短菌素进行化学修饰而合成了。多数衍生物在其截短菌素骨架的C14位上的侧链中含有一个碱性功能团。截短菌素的单对甲苯磺酸盐被用作一种通用的中间体,可通过N-、O-和S-亲核试剂来取代。