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Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors
Authors:Andrés J Ignacio  Alonso José M  Díaz Adolfo  Fernández Javier  Iturrino Laura  Martínez Pedro  Matesanz Encarna  Freyne Eddy J  Deroose Frederik  Boeckx Gustaaf  Petit Davy  Diels Gaston  Megens Anton  Somers Marijke  Van Wauwe Jean  Stoppie Paul  Cools Marina  De Clerck Fred  Peeters Danielle  de Chaffoy Didier
Institution:Janssen-Cilag, Basic Research Centre, Jarama s/n, 45007, Toledo, Spain. iandres@prodes.jnj.com
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.
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