title: Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
abstract: 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.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. james.kempson@bms.com
authors.forename: James
authors.initials: J
authors.lastname: Kempson
authors.forename: William J
authors.initials: WJ
authors.lastname: Pitts
authors.forename: Joseph
authors.initials: J
authors.lastname: Barbosa
authors.forename: Junqing
authors.initials: J
authors.lastname: Guo
authors.forename: Omonike
authors.initials: O
authors.lastname: Omotoso
authors.forename: Andrew
authors.initials: A
authors.lastname: Watson
authors.forename: Karen
authors.initials: K
authors.lastname: Stebbins
authors.forename: Gary C
authors.initials: GC
authors.lastname: Starling
authors.forename: John H
authors.initials: JH
authors.lastname: Dodd
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
authors.forename: Raymond
authors.initials: R
authors.lastname: Felix
authors.forename: Karl
authors.initials: K
authors.lastname: Fischer
mesh_terms: 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
chemical_list: D007527:Isoenzymes; D010726:Phosphodiesterase Inhibitors; D011743:Pyrimidines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7; C030986:pyrimidine