Selective cell adhesion inhibitors: Barbituric acid based α4β7—MAdCAM inhibitors

GC Harriman, M Brewer, R Bennett, C Kuhn…

Index: Harriman, Geraldine C.; Brewer, Matthias; Bennett, Robert; Kuhn, Cyrille; Bazin, Marc; Larosa, Greg; Skerker, Paul; Cochran, Nancy; Gallant, Debra; Baxter, Deborah; Picarella, Dominic; Jaffee, Bruce; Luly, Jay R.; Briskin, Michael J. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 7 p. 2509 - 2512

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Citation Number: 17

Abstract

A novel series of barbituric acid derivatives were identified as selective inhibitors of α4β7 MAdCAM (mucosal addressin cell adhesion molecule-1) interactions via a high throughput screening exercise. These inhibitors were optimized to submicromolar potencies in whole cell adhesion assays, retaining their selectivity over α4β1 VCAM.

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