Non-peptide αvβ3 antagonists.: Part 3:: Identification of potent RGD mimetics incorporating novel β-amino acids as aspartic acid replacements

被引：26

作者：

Coleman, PJ ^{[1
]}

Brashear, KM

Hunt, CA

Hoffman, WF

Hutchinson, JH

Breslin, MJ

McVean, CA

Askew, BC

Hartman, GD

Rodan, SB

Rodan, GA

Leu, CT

Prueksaritanont, T

Fernandez-Metzler, C

Ma, B

Libby, LA

Merkle, KM

Stump, GL

Wallace, AA

Lynch, JJ

Lynch, R

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 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)00666-7

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 incorporating various beta -amino acids as aspartic acid mimetics. Modification of the beta -alanine 3-substituents alters the potency and physicochemical properties of these receptor antagonists and in some cases provides orally bioavailable alpha (v)beta (3) inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：31 / 34

页数：4

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