4''-DEOXY-4''-AMINOAVERMECTINS WITH POTENT BROAD-SPECTRUM ANTIPARASITIC ACTIVITIES

被引：33

作者：

MROZIK, H

ESKOLA, P

ARISON, BH

LINN, BO

LUSI, A

MATZUK, A

SHIH, TL

TISCHLER, M

WAKSMUNSKI, FS

WYVRATT, MJ

BLIZZARD, TA

MARGIATTO, GM

FISHER, MH

SHOOP, WL

EGERTON, JR

机构：

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 20期

关键词：

D O I：

10.1016/0960-894X(95)00424-R

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Reductive amination of 4''-oxo-5-O-tert-butyldimethylsilyl-avermectins with sodium cyanoborohydride and ammonium acetate gave an epimeric mixture of 4''-deoxy-4''-amino analogs with the epimeric, axial 4''-beta-amino derivative as the major component. Acylation of the amino substituent gave highly active broad spectrum antiparasitic compounds, as determined in a sheep anthelmintic assay. 4''-Epi-acetylamino-4''-deoxyavermectin B-1(12) was selected for further antiparasitic studies and is currently under development as a novel avermectin endectocide.

引用

页码：2435 / 2440

页数：6

共 17 条

[1]

BLIZZARD T, 1990, RECENT PROGR CHEM SY

[2] SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 13-EPI-AVERMECTINS - POTENT ANTHELMINTIC AGENTS WITH AN INCREASED MARGIN OF SAFETY [J].