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Pyrazoline based MAO inhibitors: synthesis, biological evaluation and SAR studies. 2011
Monika Jagrat, and
Jagannath Behera, and
Samiye Yabanoglu, and
Ayse Ercan, and
Gulberk Ucar, and
Barij Nayan Sinha, and
Vadivelan Sankaran, and
Arijit Basu, and
Venkatesan Jayaprakash
Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India.
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.
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