Design and synthesis of novel imidazo[1,2-a]quinoxalines as PDE4 inhibitors

Abstract

New imidazo[1,2-a]quinoxaline derivatives have been synthesised by condensation of an appropriate α-aminoalcohol with a quinoxaline followed by intramolecular cyclisation and nucleophilic substitutions. Their phosphodiesterase inhibitory activities have been assessed on a preparation of the PDE4 isoform purified from a human alveolar epithelial cell line (A549). These studies showed potent inhibitory properties that emphasize the importance of a methyl amino group at position 4 and a weakly hindered group at position 1. © 2004 Elsevier Ltd. All rights reserved.