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Synthesis and biological activity of 13-epi-avermectins: potent anthelmintic agents with an increased margin of safety.

作者信息

Blizzard T A, Margiatto G M, Mrozik H, Shoop W L, Frankshun R A, Fisher M H

机构信息

Merck Sharp and Dohme Research Laboratories, Rahway, New Jersey 07065.

出版信息

J Med Chem. 1992 Oct 16;35(21):3873-8. doi: 10.1021/jm00099a014.

Abstract

Chemical conversion of the potent anthelmintic natural products avermectin B1 (1) and avermectin B2 (3) to the corresponding 13-epi analogs (15 and 9) is described. The novel analogs retain the full potency of the natural products but are substantially safer.

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