1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase  5 (PDE5) inhibitors.
1H-Pyrazolo[4,3-d]pyrimidines are a class of potent and selective second generation phosphodiesterase 5 (PDE5) inhibitors. This work explores the potency, selectivity and efficacy of 1-(2-ethoxyethyl)-1H-pyrazolo[4,5-d]pyrimidines as PDE5 inhibitors resulting in the advancement of a clinical candidate.
Tollefson
Michael B
MB
Pfizer Global Research and Development, Chesterfield, MO 63017, United States. michael.tollefson@yahoo.com
Acker
Brad A
BA
Jacobsen
E J
EJ
Hughes
Robert O
RO
Walker
John K
JK
Fox
David N A
DN
Palmer
Michael J
MJ
Freeman
Sandra K
SK
Yu
Ying
Y
Bond
Brian R
BR
D000818:Animals; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5 / Q000378:metabolism; D004285:Dogs; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D058986:Phosphodiesterase 5 Inhibitors; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D058986:Phosphodiesterase 5 Inhibitors; D011743:Pyrimidines; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5