Development of potent non-carbohydrate imidazole-based small molecule selectin inhibitors with antiinflammatory activity

…, SJ Romano, J Yu, TN Nguyen, JK John…

Index: Slee; Romano; Yu; Nguyen; John; Raheja; Axe; Jones; Ripka Journal of Medicinal Chemistry, 2001 , vol. 44, # 13 p. 2094 - 2107

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Citation Number: 82

Abstract

A novel series of non-carbohydrate imidazole-based selectin inhibitors has been discovered via high-throughput screening using a P-selectin ELISA-based assay system. The initial lead 1 had an IC50 of 17 μM in the P-selectin ELISA; this potency was significantly improved via an extensive SAR exploration. One of the current lead compounds (29) has an IC50 of 300 nM in a P-selectin ELISA; it also has good activity in P-and E-selectin cell adhesion ...