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 ...
