Synthesis and biological activities of novel 4"-alkylidene avermectin derivatives.

ID: ALA1144861

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological activities of novel 4"-alkylidene avermectin derivatives.

Authors: Nagai K, Sunazuka T, Shiomi K, Harder A, Turberg A, Omura S.

Abstract: Horner-Emmons reaction of 4"-dehydro-5-O-TBDMS-avermectin B(1a) with a variety of phosphorus ylides using LHMDS gave novel 4"-alkylidene avermectin derivatives in high yields. Further modifications led to derivatives bearing diverse functional groups. The new avermectin derivatives showed potent growth inhibitory activity against Artemia salina and Caenorhabditis elegans.

CiteXplore: 14592480

DOI: 10.1016/j.bmcl.2003.09.003

Patent ID: ┄