ChemInform Abstract: Imidazo[5,1‐f][1,2,4]triazin‐4(3H)‐ones, a New Class of Potent PDE 5 Inhibitors.

Abstract

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Cyclic GMP-Hydrolyzing Phosphodiesterases

“…The successful development of sildenafil as the first orally active and highly efficient drug for the treatment of erectile dysfunction (ED) made this structure the most widely recognized PDE5 inhibitor. Two other PDE5 inhibitors, vardenafil (Haning et al 2002) and tadalafil (Padma-Nathan et al 2001; (Haning et al 2003). Vardenafil is distinguished by its imidazotriazinone core structure which has impact on its increased potency Haning et al 2003).…”

Methyl (11aS)-1,2,3,5,11,11a-Hexahydro-3,3-dimethyl-1-oxo-6H-imidazo-[3′,4′:1,2]pyridin[3,4-b]indol-2-Substituted Acetates: Synthesis and Three-Dimensional Quantitative Structure−Activity Relationship Investigation as a Class of Novel Vasodilators

“…Thus PDE inhibitors may have a large variety of therapeutic utilities including vasodilators. , PDEs consist of 11 classes of human cyclic nucleotide phosphodiesterases, among which the PDE5 enzyme is selective for cGMP. , PDE5 is importantly expressed in human corpus cavernosum tissue . In the literature, three PDE5 inhibitors sildenafil, vardenafil, and tadalafil were reported to be capable of treating erectile dysfunction. Their structures are shown in Figure .…”

“…13,14 PDE5 is importantly expressed in human corpus cavernosum tissue. 15 In the literature, three PDE5 inhibitors sildenafil, 16 vardenafil, 17 and tadalafil 18 were reported to be capable of treating erectile dysfunction. Their structures are shown in Figure 1.…”