Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
A series of fused pyrimidine based inhibitors of PDE7 have been derived from an earlier screening lead 1. The synthesis, structure-activity relationships (SAR) and selectivity against several other PDE family members are described.
Kempson
James
J
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. james.kempson@bms.com
Pitts
William J
WJ
Barbosa
Joseph
J
Guo
Junqing
J
Omotoso
Omonike
O
Watson
Andrew
A
Stebbins
Karen
K
Starling
Gary C
GC
Dodd
John H
JH
Barrish
Joel C
JC
Felix
Raymond
R
Fischer
Karl
K
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors / Q000378:metabolism*; D002460:Cell Line; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7; D006801:Humans; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism*; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011743:Pyrimidines / Q000737:chemistry*; D013329:Structure-Activity Relationship
D007527:Isoenzymes; D010726:Phosphodiesterase Inhibitors; D011743:Pyrimidines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7; C030986:pyrimidine