2,3/18,19-DIOXIDOSQUALENE - SYNTHESIS AND ACTIVITY AS A POTENT INHIBITOR OF 2,3-OXIDOSQUALENE-LANOSTEROL CYCLASE IN RAT-LIVER MICROSOMES

被引：18

作者：

ABAD, JL ^{[1
]}

CASAS, J ^{[1
]}

SANCHEZBAEZA, F ^{[1
]}

MESSEGUER, A ^{[1
]}

机构：

[1] CSIC,CID,DPT BIOL ORGAN CHEM,J GIRONA 18,E-08034 BARCELONA,SPAIN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 10期

关键词：

2,3/18,19-DIOXIDOSQUALENE; INHIBITION; 2,3-OXIDOSQUALENE-LANOSTEROL CYCLASE (EC 5.4.99.7);

D O I：

10.1016/S0960-894X(00)80221-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2,3:18,19-Dioxidosqualene (3) was synthesized and isolated as a diastereomeric mixture. Incubation of 2,3-oxidosqualene with rat liver microsomes in the presence of dioxide 3 caused a high inhibition of lanosterol production (K(i) = 0. 11 muM). The kinetic data showed that this inhibition was noncompetitive.

引用

页码：1239 / 1242

页数：4

共 12 条

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