Non-peptide αvβ3 antagonists.: Part 4:: Potent and orally bioavailable chain-shortened RGD mimetics

被引：33

作者：

Coleman, PJ ^{[1
]}

Askew, BC

Hutchinson, JH

Whitman, DB

Perkins, JJ

Hartman, GD

Rodan, GA

Leu, CT

Prueksaritanont, T

Fernandez-Metzler, C

Merkle, KM

Lynch, R

Lynch, JJ

Rodan, SB

Duggan, ME

机构：

[1] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA

[2] Merck Res Labs, Dept Bone Biol & Osteoporosis Res, W Point, PA 19486 USA

[3] Merck Res Labs, Dept Drug Metab, W Point, PA 19486 USA

[4] Merck Res Labs, Dept Pharmacol, W Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(02)00396-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potent non-peptidic alpha(v)beta(3) antagonists have been prepared where deletion of an amide bond from an earlier series of linear RGD-mimetics provides a novel series of chain-shortened alpha(v)beta(3) antagonists with significantly improved oral pharmacokinetics. These chain-shortened alpha(v)beta(3) antagonists represent structurally novel integrin inhibitors. (C) 2002 Published by Elsevier Science Ltd.

引用

页码：2463 / 2465

页数：3

共 17 条

[1] SYNTHESIS OF HETEROCYCLIC BETA-AMINO ACIDS - A CONVENIENT PREPARATION OF BETA-AMINO-5-PYRIMIDINEPROPANOIC ACID AND DERIVATIVES [J].