title: The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
abstract: This communication describes the synthesis and in vitro evaluation of a novel and potent series of phosphodiesterase type IV (PDE4) inhibitors. The compounds described represent conformationally constrained analogues of RP 73401, Piclamilast. Preliminary evidences of reduced side effects of II compared to standards are also reported.
authors.affiliation: Inpharzam Ricerche, Zambon Group, Cadempino, Switzerland. mauro.napoletano@zambongroup.com
authors.forename: M
authors.initials: M
authors.lastname: Napoletano
authors.forename: G
authors.initials: G
authors.lastname: Norcini
authors.forename: F
authors.initials: F
authors.lastname: Pellacini
authors.forename: F
authors.initials: F
authors.lastname: Marchini
authors.forename: G
authors.initials: G
authors.lastname: Morazzoni
authors.forename: P
authors.initials: P
authors.lastname: Ferlenga
authors.forename: L
authors.initials: L
authors.lastname: Pradella
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010793:Phthalazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D020889:Rolipram / Q000737:chemistry / Q000494:pharmacology
chemical_list: C419206:1-(3,5-dichloropyrid-4-ylmethyl)-5-cyclopentoxy-6-methoxyphthalazine; D001549:Benzamides; D010726:Phosphodiesterase Inhibitors; D010793:Phthalazines; D011725:Pyridines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D020889:Rolipram; C087566:piclamilast