Reddy, G. Lakshma published the artcileDesign, synthesis and biological evaluation of pyrazolopyrimidinone based potent and selective PDE5 inhibitors for treatment of erectile dysfunction, Application In Synthesis of 73874-95-0, the main research area is pyrazolopyrimidinone PDE5 inhibitor erectile dysfunction; Erectile dysfunction; PDE5 inhibitors; PDE6 enzyme; Pyrazolopyrimidinone derivatives; Sildenafil.
The authors’ previous discovery of series of pyrazolopyrimidinone based PDE5 inhibitors led to find potent leads but with low aqueous solubility and poor bioavailability, and low selectivity. Now, a new series of same pyrazolopyrimidinone scaffold is designed, synthesized and evaluated for its PDE5 inhibitory potential. Some of the mols. are found more potent and selective PDE5 inhibitors in vitro than sildenafil. The studies revealed that compound 5 is 20 fold selective to PDE5 against PDE6. As PDE6 enzyme is involved in the phototransduction pathway in the retina and creates distortion problem, the selectivity for PDE5 specifically against PDE6 enzyme is preferred for any development candidate and in present study, compound 5 is devoid of this liability of selectivity issue. Moreover, compound 5 showed excellent in vivo efficacy in conscious rabbit model, it’s almost comparable to sildenafil. The preclin. pharmacol. including pharmacokinetic and physicochem. parameter studies were also performed for compound 5, it has good PK properties and other physicochem. parameters. The development of these selective PDE5 inhibitors can further lead to draw strategies for the novel preclin. and/or clin. candidates based on pyrazolopyrimidinone scaffold.
Bioorganic Chemistry published new progress about Erectile dysfunction. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Application In Synthesis of 73874-95-0.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem