Senga, Keitaro; O’Brien, Darrell E.; Scholten, Mieka B.; Novinson, Thomas; Miller, Jon P.; Robins, Roland K. published the artcile< Synthesis and enzymic activity of various substituted pyrazolo[1,5-a]-1,3,5-triazines as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors>, COA of Formula: C6H5ClN4S, the main research area is pyrazolotriazine cAMP phosphodiesterase inhibitor preparation; pyrazolylamidine cyclization; amidine pyrazolyl cyclization.
I (R1 = H, Me, Et, SMe; R2 = H, Ph, Pr, SMe, NHEt, NHBu, NEt2 piperidino, OH, NHPr, SH, OCHMe2, Me, SEt, OMe, OPr; R3 = Ph, C6H4OMe-4, H; R4 = H, Br, C6H4Me-3, Ph, cyano, CO2Et, Cl), prepared by cyclizing II with (R2CO)2O or R2C(OEt)3, followed by electrophilic substitution in the pyrazole ring and/or nucleophilic substitution in the 1,3,5-triazine moiety, were studied as inhibitors of cAMP phosphodiesterase (PDE) isolated from bovine brain, bovine heart, and rabbit lung. A number of compounds were superior to theophylline. 2-Ethyl-7-phenylpyrazolo[1,5-a]-1,3,5-triazine was 97 times more potent than theophylline as an inhibitor of bovine brain PDE. 8-Bromo-2,4-dimethyl-7-phenylpyrazolo[1,5-a]-1,3,5-triazine showed αlung = 40 compared to αheart = 3.0. Thus, various substituents could increase or decrease the inhibition relative to the type and source of tissue from which the PDE was isolated. The most active compound was 8-bromo-4-(diethylamino)-7-phenylpyrazolo[1,5-a]-1,3,5-triazine which was 185 times more potent than theophylline as an inhibitor of PDE isolated from rabbit lung. Structure-activity relationships were reviewed.
Journal of Medicinal Chemistry published new progress about Structure-activity relationship. 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, COA of Formula: C6H5ClN4S.
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics