Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
A series of purine based inhibitors of PDE7 has been derived from screening lead 1a. The synthesis, structure-activity relationships (SAR), and selectivity against several other PDE family members are described.
Pitts
William J
WJ
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. pittsw@bms.com
Vaccaro
Wayne
W
Huynh
Tram
T
Leftheris
Katerina
K
Roberge
Jacques Y
JY
Barbosa
Joseph
J
Guo
Junqing
J
Brown
Baerbel
B
Watson
Andrew
A
Donaldson
Karen
K
Starling
Gary C
GC
Kiener
Peter A
PA
Poss
Michael A
MA
Dodd
John H
JH
Barrish
Joel C
JC
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D001665:Binding Sites; D002460:Cell Line; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000201:enzymology
D004791:Enzyme Inhibitors; D008024:Ligands; D011687:Purines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7