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

Pyrazoline
Rat liver enzyme
MAO isoform
Selectivity
Inhibitors

How to Cite

(1)
Badavath, V. N.; Singh, A. K.; Jadav, S. S.; Mishra, N.; Dev, A.; Sinha, B. N.; Jayaprakash, V. Pyrazoline Carboxylates As Selective MAO-B Inhibitors: Synthesis and Biological Screening. J Pharm Chem 2015, 2 (1), 1-5. https://doi.org/10.14805/jphchem.2015.art35.

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.

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