Pyrazoline based MAO inhibitors: Synthesis, biological evaluation and SAR studies

JAGRAT, Monika; BEHERA, Jagannath; YABANOGLU, Samiye; ERCAN, AYŞE; UÇAR, GÜLBERK; SINHA, Barij; SANKARAN, Vadivelan; BASU, Arijit; JAYAPRAKASH, Venkatesan

doi:10.1016/j.bmcl.2011.05.057

Pyrazoline based MAO inhibitors: Synthesis, biological evaluation and SAR studies

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JAGRAT M., BEHERA J., YABANOGLU S., ERCAN A., UÇAR G., SINHA B. N., ...More

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol.21, no.14, pp.4296-4300, 2011 (SCI-Expanded)

Publication Type: Article / Article
Volume: 21 Issue: 14
Publication Date: 2011
Doi Number: 10.1016/j.bmcl.2011.05.057
Journal Name: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
Page Numbers: pp.4296-4300
Hacettepe University Affiliated: Yes

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. (C) 2011 Elsevier Ltd. All rights reserved.