title: Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.
abstract: The following letter presents the synthesis and in vitro evaluation of a novel quaternary substituted series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds represent conformationally constrained analogues of the Celltech PDE IV inhibitor, CDP 840. Examples with sub-micromolar IC50's for PDE4 inhibition are reported.
authors.affiliation: Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA.
authors.forename: C
authors.initials: C
authors.lastname: Hulme
authors.forename: G B
authors.initials: GB
authors.lastname: Poli
authors.forename: F C
authors.initials: FC
authors.lastname: Huang
authors.forename: J E
authors.initials: JE
authors.lastname: Souness
authors.forename: S W
authors.initials: SW
authors.lastname: Djuric
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D010726:Phosphodiesterase Inhibitors; D011725:Pyridines; C102660:CDP 840; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4