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Bioorg Med Chem Lett. 2011 Jul 15;21(14):4296-300. doi: 10.1016/j.bmcl.2011.05.057. Epub 2011 May 25.

Pyrazoline based MAO inhibitors: synthesis, biological evaluation and SAR studies.

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  • 1Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India.

Abstract

Twenty-two pyrazoline derivatives were synthesized and tested for their human MAO (hMAO) inhibitory activity. Twelve molecules with unsubstituted ring A and substituted ring C (5-16) were found to be potent inhibitors of hMAO-A isoform with SI(MAO-A) in the order 10(3) and 10(4). Ten molecules with unsubstituted ring A and without ring C (21-30), in which eight molecules (21, 23-26, and 28-30) were selective for hMAO-A, one for hMAO-B (22) and the other one non-selective (27). Presence of ring C increases potency as well as SI towards hMAO-A; however its absence decreases both potency and SI towards hMAO-A and hMAO-B.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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