Heterocyclic ring scaffolds as small-molecule cholesterol absorption inhibitors

被引：26

作者：

Ritter, T

Kvaerno, L

Werder, M

Hauser, H

Carreira, EM ^{[1
]}

机构：

[1] ETH Honggerberg, Organ Chem Lab, CH-8093 Zurich, Switzerland

[2] Lipideon Biotechnol AG, CH-8713 Uerikon, Switzerland

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2005年 / 3卷 / 19期

关键词：

D O I：

10.1039/b510100j

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Enantio- and diastereoselective syntheses of a substituted oxazolidinone, isoxazoline and pyrazoline as beta-lactam surrogates are described. The substituted heterocycles were designed to incorporate side chains closely resembling those found in the beta-lactam cholesterol absorption inhibitor ezetimibe (1). Additionally, the in vitro inhibitory efficacy of the novel compounds as cholesterol absorption inhibitors is reported using a brush border membrane vesicle assay.

引用

页码：3514 / 3523

页数：10

共 49 条

[1]

BANSAL RK, 1988, J INDIAN CHEM SOC, V65, P134

[2] HORNER-WADSWORTH-EMMONS REACTION - USE OF LITHIUM-CHLORIDE AND AN AMINE FOR BASE SENSITIVE COMPOUNDS [J].