1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.

作者：Tollefson Michael B^*; Acker Brad A; Jacobsen E J; Hughes Robert O; Walker John K; Fox David N A; Palmer Michael J; Freeman Sandra K; Yu Ying; Bond Brian R

来源：Bioorganic and Medicinal Chemistry Letters, 2010, 20(10): 3125-3128.

DOI：10.1016/j.bmcl.2010.03.106

1H-Pyrazolo[4,3-d]pyrimidines were previously disclosed as a potent second generation class of phosphodiesterase 5 (PDE5) inhibitors. This work explores the advancement of more selective and potent PDE5 inhibitors resulting from the substitution of 2-(2,2,2-trifluoroethoxy)ethyl at the 1 position in the so-called alkoxy pocket.