Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors

…, E Matesanz, EJ Freyne, F Deroose, G Boeckx…

Index: 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 Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 4 p. 653 - 658

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Citation Number: 26

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 ...

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[Christensen, Siegfried B.; Guider, Aimee; Forster, Cornelia J.; Gleason, John G.; Bender, Paul E.; Karpinski, Joseph M.; Dewolf Jr., Walter E.; Barnette, Mary S.; Underwood, David C.; Griswold, Don E.; Cieslinski, Lenora B.; Burman, Miriam; Bochnowicz, Steven; Osborn, Ruth R.; Manning, Carol D.; Grous, Marilyn; Hillegas, Leonard M.; Bartus, Joan O'Leary; Dominic Ryan; Eggleston, Drake S.; Curtis Haltiwanger; Torphy, Theodore J. Journal of Medicinal Chemistry, 1998 , vol. 41, # 6 p. 821 - 835]