Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships

James Kempson; William J Pitts; Joseph Barbosa; Junqing Guo; Omonike Omotoso; Andrew Watson; Karen Stebbins; Gary C Starling; John H Dodd; Joel C Barrish; Raymond Felix; Karl Fischer

doi:10.1016/j.bmcl.2005.02.025

Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1829-33. doi: 10.1016/j.bmcl.2005.02.025.

Authors

James Kempson¹, William J Pitts, Joseph Barbosa, Junqing Guo, Omonike Omotoso, Andrew Watson, Karen Stebbins, Gary C Starling, John H Dodd, Joel C Barrish, Raymond Felix, Karl Fischer

Affiliation

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

PMID: 15780616
DOI: 10.1016/j.bmcl.2005.02.025

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.

MeSH terms

3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors
3',5'-Cyclic-AMP Phosphodiesterases / metabolism*
Cell Line
Cyclic Nucleotide Phosphodiesterases, Type 7
Humans
Inhibitory Concentration 50
Isoenzymes / antagonists & inhibitors
Isoenzymes / metabolism*
Phosphodiesterase Inhibitors / chemical synthesis*
Phosphodiesterase Inhibitors / pharmacology
Pyrimidines / chemistry*
Structure-Activity Relationship

Substances

Isoenzymes
Phosphodiesterase Inhibitors
Pyrimidines
3',5'-Cyclic-AMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 7
pyrimidine