Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis

ACS Medicinal Chemistry Letters
Vishnu N BadavathVenkatesan Jayaprakash

Abstract

A series of new 2-methoxy-4-(5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)phenolderivatives, 4-13, were synthesized and tested for their human MAO inhibitory activity. All the compounds were found to be selective and reversible toward hMAO-A except 4, a selective inhibitor of hMAO-B and 12, a nonselective inhibitor. Compound 7 was found to be a potent inhibitor of hMAO-A with Ki = 0.06 ± 0.003 μM and was having selectivity index of (SI = 1.02 × 10(-5)). It was found to be better than standard drug, Moclobemide (hMAO-A with Ki = 0.11 ± 0.01 μM) with selectivity index of SI = 0.049. Molecular docking simulation was carried out to understand the crucial interactions responsible for selectivity and potency.

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Citations

Jun 6, 2016·International Journal of Biological Macromolecules·Bijo MathewVenkatesan Jayaprakash
Apr 4, 2017·Journal of Natural Products·Yun-Song WangXiao-Jiang Hao
Jan 18, 2019·Current Computer-aided Drug Design·Ravi JarapulaSarangapani Manda
Jan 4, 2019·Medicinal Research Reviews·Rati Kailash Prasad Tripathi, Senthil Raja Ayyannan
Aug 16, 2018·MedChemComm·Chandrani NathVenkatesan Jayaprakash
Nov 21, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Muhammed ÇeçenHoon Kim
Jun 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Aathira Sujathan NairHoon Kim
Oct 14, 2020·ACS Combinatorial Science·Ashique PalakkathondiBijo Mathew
Mar 6, 2019·The Journal of Physical Chemistry. a·Marzieh SoltaniHassan Sabzyan
Oct 9, 2018·Journal of Agricultural and Food Chemistry·Ruige YangHui Xu

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