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

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Jagrat M, Behera J, Yabanoglu S, Ercan A, Ucar G, Sinha BN, Sankaran V, Basu A, Jayaprakash V

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

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

PubMed ID

21680183 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Moclobemide	Amine oxidase [flavin-containing] A	Ki (nM)	5	N/A	N/A	Details
Moclobemide	Amine oxidase [flavin-containing] B	Ki (nM)	1080	N/A	N/A	Details
Selegiline	Amine oxidase [flavin-containing] A	Ki (nM)	9060	N/A	N/A	Details
Selegiline	Amine oxidase [flavin-containing] B	Ki (nM)	91	N/A	N/A	Details