Journal of medicinal chemistry

Synthesis and cyclic GMP phosphodiesterase inhibitory activity of a series of 6-phenylpyrazolo [3, 4-d] pyrimidones

B Dumaître, N Dodic

Index: Dumaitre, Bernard; Dodic, Nerina Journal of Medicinal Chemistry, 1996 , vol. 39, # 8 p. 1635 - 1644

Full Text: HTML

Citation Number: 60

Abstract

A series of 6-phenylpyrazolo [3, 4-d] pyrimidones is described which are specific inhibitors of cGMP specific (type V) phosphodiesterase. Enzymatic and cellular activity as well as in vivo oral antihypertensive activity are evaluated. A n-propoxy group at the 2-position of the phenyl ring is necessary for activity. A series of products substituted at the 5-position in addition to the 2-n-propoxy was prepared and evaluated. This position can accommodate ...