Sildenafil (VIAGRATM), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction

Crystal structure of ethyl-5-methyl-1-(pyridin-3-yl)-1H-pyrazole-4-carboxylate-(dibenzoylmethane), C17H15N4O

“…The pyrazole ring is present in numerous pharmacologically and agrochemically important compounds, such as inhibitors of HIV-1 reverse transcriptase [1],hypocholesterolemic activity [2]and elective inhibition of cyclooxygenase-2 (COX-2) [3].Several compounds of this type act as antagonists of the receptor, which is present on the surface of many tumorcells [4]. Others are important agrochemicals used,e.g., as insecticides [5].Ofparticularimportanceasa pharmacophore, the N-substituented pyrazole derivatives form part of several drugs such as the antidepressant Zometapine [6], the inhibitor of type 5c GMP phosphodiesterase Sildenafil [7], and the antibacterial agent FR21818 [8]. Good examples of the usefulness of this same unit in the preparation of insecticides and acaricides include the pesticides Tebufenpyrad [9]Tolfenpyrad [10] and Cyanopyrafen [11].…”

Pharmacological properties of cashew (Anacardium occidentale)

“…Through a virtual evaluation, it was found that anacardic acid could be fitted into the aurora kinase enzyme A and B; and thus, could activate the aurora kinase A-mediated phosphorylation of histone H3 by modifying the structure of the enzyme and increasing its activity (Kishore et al, 2008). The drug sildenafil (VIAGRA) is a potent inhibitor of 5-fosfadiesterase (Terrett et al, 1996). This is the key enzyme used for the regulation of smooth muscle tone, playing an important role in erectile dysfunction (Beavo and Reifsnyder, 1990).…”

How Psychiatrists Can Build New Therapies for Impotence

“…The strategy of phosphodiesterase inhibition has three potential advantages [7][8][9] : it allows oral administration; it leads to erections during physiologic sexual arousal (not requiring on-demand mechanics); and it boosts the most common type of problem, namely partial, intermittent erectile dysfunction of multifactorial causation.…”