The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
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.
Napoletano
M
M
Inpharzam Ricerche, Zambon Group, Cadempino, Switzerland. mauro.napoletano@zambongroup.com
Norcini
G
G
Pellacini
F
F
Marchini
F
F
Morazzoni
G
G
Ferlenga
P
P
Pradella
L
L
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
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