Pyrazoline carboxylates as selective MAO-B inhibitors: Synthesis and Biological screening

Vishnu Nayak Badavath, Alok Kumar Singh, Surender Singh Jadav, Nibha Mishra, Abhimanyu Dev, Barij Nayan Sinha, Venkatesan Jayaprakash

Abstract


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.


Keywords


Pyrazoline; Rat liver enzyme; MAO isoform; Selectivity; Inhibitors; Rat liver enzyme; MAO isoform; Selectivity; Inhibitors

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References


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DOI: http://dx.doi.org/10.14805/jphchem.2015.art35

DOI (PDF): http://dx.doi.org/10.14805/jphchem.2015.gal24

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