CHEMICAL MODIFICATION AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF PYRIPYROPENES - POTENT, BIOAVAILABLE INHIBITOR OF ACYL-COA-CHOLESTEROL O-ACYLTRANSFERASE (ACAT)

被引：33

作者：

OBATA, R

SUNAZUKA, T

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：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 22期

关键词：

D O I：

10.1016/0960-894X(95)00451-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Modification and structure-activity relationships of ACAT inhibitor pyripyropene were examined. PR-109 (7g) showed the most potent (IC50 = 6 nM) inhibitory activity. PR-86 (2e) also had strong inhibitory activity (IC50 = 19 nM) and its in vivo activity improved 10 times better (ED(50) = 10 mg/kg) than that of pyripyropene A.

引用

页码：2683 / 2688

页数：6

共 11 条

[1]

CHANG TY, 1983, ENZYMES, V16, P523

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