Author/Authors :
J. Ignacio Andrés، نويسنده , , José M. Alonso-Meijide، نويسنده , , Adolfo D?az، نويسنده , , Javier Fernandez-Suarez، نويسنده , , Laura Iturrino، نويسنده , , Pedro Martinez Arbizu، نويسنده , , Encarna Matesanz، نويسنده , , Eddy J. Freyne، نويسنده , , Frederik Deroose، نويسنده , , Gustaaf Boeckx، نويسنده , , Davy Petit، نويسنده , , Gaston Diels، نويسنده , , Anton Megens، نويسنده , , Marijke Somers، نويسنده , , Jean Van Wauwe، نويسنده , , Paul Stoppie، نويسنده , , Marina Cools، نويسنده , , Fred De Clerck، نويسنده , , Danielle Peeters، نويسنده , , Didier de Chaffoy، نويسنده ,
Abstract :
This communication describes the synthesis and in vitro PDE4 inhibitory activity of a novel series of imidazol-2-one and 2-cyanoiminoimidazole derivatives. The compounds described were also tested in in vivo models to evaluate their anti-inflammatory activity after topical administration as well as their gastro-intestinal side effects. Several compounds proved to be potent PDE4 inhibitors and some 2-cyanoiminoimidazoles showed less pronounced gastro-intestinal side effects than reference compounds but maintained anti-inflammatory activity after topical administration.
