183659-72-5Relevant articles and documents
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
Andres, J Ignacio,Alonso, Jose M,Diaz, Adolfo,Fernandez, Javier,Iturrino, Laura,Martinez, 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
, p. 653 - 658 (2007/10/03)
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.