灰黄霉素类似物的合成及生物活性

Synthesis and biological activities of griseofulvin analogs.

作者信息

Ko B S, Oritani T, Yamashita K

机构信息

Department of Agricultural Chemistry, Tohoku University, Sendai, Japan.

出版信息

Agric Biol Chem. 1990 Sep;54(9):2199-204.

PMID:1368574

Abstract

In order to elucidate the structure-activity relationship of griseofulvin (1), (+/-)-6-demethyl analog (3), 2-demethoxy-6-demethyldihydro analog (4), (+/-)-dechloro-6-ethyl analog (5), (+/-)-dechloro-6-epi-ethyl analog (6), (+/-)6-ethyl analog (7) and (+/-)-6-epi-ethyl analog (8) were synthesized by a Diels-Alder cycloaddition of alkylidene ketones (16, 17 18, 19 and 20) with modified 1,3-butadienes (21 or 22). Their biological activities were examined against fungi.

摘要

为阐明灰黄霉素（1）、（±）-6-去甲基类似物（3）、2-去甲氧基-6-去甲基二氢类似物（4）、（±）-去氯-6-乙基类似物（5）、（±）-去氯-6-表乙基类似物（6）、（±）-6-乙基类似物（7）和（±）-6-表乙基类似物（8）的构效关系，通过亚烷基酮（16、17、18、19和20）与修饰的1,3-丁二烯（21或22）的狄尔斯-阿尔德环加成反应合成了这些化合物。检测了它们对真菌的生物活性。