Pyrazoline carboxylates as selective MAO-B inhibitors: Synthesis and Biological screening
A series of carboxylates of pyrazolines ( 3a-3h ) were synthesized from ethyl 2-benzylidene-3-oxobutanoate esters using hydrazine hydrate and ethanol as solvent. All the compounds ( 3a-3h ) screened for their MAO inhibitory activity using rat brain MAO. All the compounds were found to be selective, reversible and competitive inhibitors of MAO-B except compound 3d and 3h which was found to be non-selective. These compounds were found to be active against MAO-B at concentration close to 1 ?M ( 3e = 0.99 ?M, 3a = 0.92 ?M and 3b = 1.11?M). Compound 3a was potent amongst these while 3b was more selective towards MAO-B with selectivity index 2.88.
