New imidazo[1,2-a]quinoxaline derivatives have been synthesised by condensation of an appropriate alpha-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.
Pharmacochimie et Biomolécules, Laboratoire de Chimie Organique Pharmaceutique, Faculté de Pharmacie, 15, Av. Ch. Flahault, BP 14 491, 34093 Montpellier Cedex 5, France.
