SYNTHESIS OF 5-KETO-5-OXIME DERIVATIVES OF MILBEMYCINS AND THEIR ACTIVITIES AGAINST MICROFILARIAE

被引：33

作者：

TSUKAMOTO, Y ^{[1
]}

SATO, K ^{[1
]}

MIO, S ^{[1
]}

SUGAI, S ^{[1
]}

YANAI, T ^{[1
]}

KITANO, N ^{[1
]}

MURAMATSU, S ^{[1
]}

NAKADA, Y ^{[1
]}

IDE, J ^{[1
]}

机构：

[1] SANKYO CO LTD,MED CHEM RES LABS,SHINAGAWA KU,TOKYO 140,JAPAN

来源：

AGRICULTURAL AND BIOLOGICAL CHEMISTRY | 1991年 / 55卷 / 10期

关键词：

D O I：

10.1080/00021369.1991.10870993

中图分类号：

S3 [农学（农艺学）];

学科分类号：

0901 ;

摘要：

Starting from milbemycin D (1), milbemycin A4 (2) and milbemycin A3 (3), a series of 5-keto-5-oxime derivatives were synthesized by selective oximation at the alpha,beta-conjugated carbonyl function of the 5-ketomilbemycins (4-6). The activities of the synthesized compounds were studied in dogs naturally infested with microfilariae of Dirofilaria immitis. The 5-keto-5-oximes of milbemycin D (7), A4 (8) and A3 (9) had quite high efficacy to control the microfilariae and more potency than their parents, while the 5-O-acyl oximes (11-15) also exhibited high activity.

引用

页码：2615 / 2621

页数：7

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