title: Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams.
abstract: This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE IV) inhibitors. Several of the quaternary substituted lactams presented possess low nanomolar IC50's for PDE IV inhibition.
authors.affiliation: Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA.
authors.forename: C
authors.initials: C
authors.lastname: Hulme
authors.forename: K
authors.initials: K
authors.lastname: Moriarty
authors.forename: F C
authors.initials: FC
authors.lastname: Huang
authors.forename: J
authors.initials: J
authors.lastname: Mason
authors.forename: D
authors.initials: D
authors.lastname: McGarry
authors.forename: R
authors.initials: R
authors.lastname: Labaudiniere
authors.forename: J
authors.initials: J
authors.lastname: Souness
authors.forename: S
authors.initials: S
authors.lastname: Djuric
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D007769:Lactams / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D007769:Lactams; D010726:Phosphodiesterase Inhibitors; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4