Identification of purine inhibitors of phosphodiesterase 7 (PDE7)

William J Pitts; Wayne Vaccaro; Tram Huynh; Katerina Leftheris; Jacques Y Roberge; Joseph Barbosa; Junqing Guo; Baerbel Brown; Andrew Watson; Karen Donaldson; Gary C Starling; Peter A Kiener; Michael A Poss; John H Dodd; Joel C Barrish

doi:10.1016/j.bmcl.2004.03.021

Identification of purine inhibitors of phosphodiesterase 7 (PDE7)

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2955-8. doi: 10.1016/j.bmcl.2004.03.021.

Authors

William J Pitts¹, Wayne Vaccaro, Tram Huynh, Katerina Leftheris, Jacques Y Roberge, Joseph Barbosa, Junqing Guo, Baerbel Brown, Andrew Watson, Karen Donaldson, Gary C Starling, Peter A Kiener, Michael A Poss, John H Dodd, Joel C Barrish

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. pittsw@bms.com

PMID: 15125967
DOI: 10.1016/j.bmcl.2004.03.021

Abstract

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.

MeSH terms

3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
Binding Sites
Cell Line
Cyclic Nucleotide Phosphodiesterases, Type 7
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology
Humans
Inhibitory Concentration 50
Ligands
Purines / chemical synthesis*
Purines / pharmacology*
Structure-Activity Relationship
T-Lymphocytes / enzymology

Substances

Enzyme Inhibitors
Ligands
Purines
3',5'-Cyclic-AMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 7