Chemical modification and structure-activity relationships of pyripyropenes .2. 1,11-cyclic analogs

被引：26

作者：

Obata, R

Sunazuka, T

Kato, Y

Tomoda, H

Harigaya, Y

Omura, S

机构：

[1] KITASATO INST,BIOL FUNCT RES CTR,MINATO KU,TOKYO 108,JAPAN

[2] KITASATO UNIV,SCH PHARMACEUT SCI,MINATO KU,TOKYO 108,JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1996年 / 49卷 / 11期

关键词：

D O I：

10.7164/antibiotics.49.1149

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

A series of 1,11-cyclic analogs of pyripyropene A were prepared. Replacement of the 1,11-acyl groups of pyripyropenes with 1,11-cyclic acetals effectively improved in vitro acyl CoA:cholesterol acyltransferase (ACAT) inhibitory activity. Especially noteworthy is benzylidene acetal analog 35, the most potent inhibitor (IC50 = 5.6 nM) among the derivatives prepared so far, which showed 16 times more potent inhibitory activity than pyripyropene A.

引用

页码：1149 / 1156

页数：8

共 6 条

[1] PREPARATION AND PROPERTIES OF STEROIDAL 17,20- AND 20,21-ACETONIDES EPIMERIC AT C-20 .I. DERIVATIVES OF 5BETA-PREGNAN-3ALPHA-O1 [J].