Microwave-assisted synthesis of a series of 4,5-dihydro-1H-pyrazoles endowed with selective COX-1 inhibitory potency

Considerable efforts have been directed towards the discovery of selective cyclooxygenase isoxyme 1 (COX-1) inhibitors due to recent work highlighting involvement COX-1 in pathogenesis pain, neuroinflammation, cancer and cardiovascular disorders. In this context, paper aims describe 2-pyrazolines endowed with inhibitory potency. An efficient microwave-assisted synthetic method was applied for preparation a series pyrazolines, which were tested their 2 (COX-2) effects using colorimetric assay. The cytotoxic properties most potent derivatives on NIH/3T3 fibroblast cells determined MTT method. 1-(3-Fluorophenyl)-5-(3,4-methylendioxyphenyl)- 3-(2-thienyl)-4,5-dihydro-1H-pyrazole (2g) 1-(3-bromophenyl)- 5-(3,4-methylendioxyphenyl)-3-(2-thienyl)-4,5-dihydro-1H-pyrazole (2h) as inhibitors. According silico data obtained from Schr?dinger?s QikProp module, both compounds are estimated possess favourable oral bioavailability drug-likeness. This could be rational guideline further modifications at different sites 2-pyrazoline motif bring out new class