Synthesis of novel pyrazolopyrrolopyrazines, potential analogs of sildenafil

M Kopp, JC Lancelot, P Dallemagne…

Index: Kopp; Lancelot; Dallemagne; Rault Journal of Heterocyclic Chemistry, 2001 , vol. 38, # 5 p. 1045 - 1050

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Citation Number: 69

Abstract

Sildenafil [1] (1, VIAGRA®, Scheme 1) is a potent inhibitor of phosphodiesterase type 5 (PDE 5) [2] whose effectiveness in treating male erectile dysfunction was recently discovered. PDE5 is the primary cGMP hydrol- yzing enzyme present in the corpus cavernosal smooth muscle of the penis. Upon sexual stimulation, nitric oxyde (NO) is released and activates guanylyl cyclase which pro- duces cGMP [3]. The latter initiates a protein phosphoryla- tion cascade that ...