Selwood, David L. published the artcileSynthesis and Biological Evaluation of Novel Pyrazoles and Indazoles as Activators of the Nitric Oxide Receptor, Soluble Guanylate Cyclase, HPLC of Formula: 27412-71-1, the main research area is pyrazole indazole preparation activator nitric oxide receptor guanylate cyclase; guanylate cyclase activator dimethylaminopropyloxy pyrazole derivative; benzydamine analog preparation potent inhibitor platelet aggregation.
Database searching and compound screening identified 1-benzyl-3-(3-dimethylaminopropyloxy)indazole (benzydamine) as a potent activator of the nitric oxide receptor, soluble guanylate cyclase. A comprehensive structure-activity relationship study surrounding benzydamine clearly showed that the indazole C-3 dimethylaminopropyloxy substituent was critical for enzyme activity. However replacement of the indazole ring of benzydamine by appropriately substituted pyrazoles maintained enzyme activity. Compounds were evaluated for inhibition of platelet aggregation and showed a general lipophilicity requirement. Aryl-substituted pyrazoles I (R = CH2Ph, R1 = CONHC6H4OMe-p; R = CH2Ph, R1 = Ph; R = Ph, R1 = Ph) demonstrated potent activation of soluble guanylate cyclase and potent inhibition of platelet aggregation. Pharmacokinetic studies in rats showed that I (R = CH2Ph, R1 = CONHC6H4OMe-p) exhibits modest oral bioavailability (12%). Furthermore I (R = CH2Ph, R1 = CONHC6H4OMe-p) has an excellent selectivity profile notably showing no significant inhibition of phosphodiesterases or nitric oxide synthases.
Journal of Medicinal Chemistry published new progress about Drug bioavailability. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, HPLC of Formula: 27412-71-1.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics