Microsomal triglyceride transfer protein inhibitors: Discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents

被引：16

作者：

Magnin, DR ^{[1
]}

Biller, SA

Wetterau, J

Robl, JA

Dickson, JK

Taunk, P

Harrity, TW

Lawrence, RM

Sun, CQ

Wang, T

Logan, J

Fryszman, O

Connolly, F

Jolibois, K

Kunselman, L

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Chem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Metab Dis, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(03)00116-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of newly synthesized phosphonate esters were evaluated for their effects on microsomal triglyceride transfer protein activity (MTP). The most potent compounds were evaluated for their ability to inhibit lipoprotein secretion in HepG2 cells and to affect VLDL secretion in rats. These inhibitors were also found to lower serum cholesterol levels in a hamster model upon oral dosing. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1337 / 1340

页数：4

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