title: New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
abstract: Pharmacophoric comparison between papaverine and tofisopam led to identify three new series of micro- to sub-micromolar inhibitors of phosphodiesterase-4, including 7,8-dialkoxy-2,3-benzodiazepin-4-one derivatives, 7,8-dialkoxy-1,4-benzodiazepin-2-one derivatives, and dialkoxybenzophenone derivatives.
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200, CNRS, Université de Strasbourg, Faculté de Pharmacie, 74 route du Rhin, 67400 Illkirch Graffenstaden, France. fbihel@unistra.fr
authors.forename: Frédéric J J
authors.initials: FJ
authors.lastname: Bihel
authors.forename: Hélène
authors.initials: H
authors.lastname: Justiniano
authors.forename: Martine
authors.initials: M
authors.lastname: Schmitt
authors.forename: Malik
authors.initials: M
authors.lastname: Hellal
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Ibrahim
authors.forename: Claire
authors.initials: C
authors.lastname: Lugnier
authors.forename: Jean-Jacques
authors.initials: JJ
authors.lastname: Bourguignon
mesh_terms: D001569:Benzodiazepines / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D010208:Papaverine / Q000737:chemistry / Q000494:pharmacology*; D058988:Phosphodiesterase 4 Inhibitors / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D058988:Phosphodiesterase 4 Inhibitors; D001569:Benzodiazepines; D010208:Papaverine; C012582:tofisopam