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

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.

Graphical abstractA 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 other integrins.Figure optionsDownload full-size imageDownload as PowerPoint slide