title: Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis.
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.
authors.affiliation: Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology , Mesra, Ranchi, Jharkhand 835 215, India.
authors.forename: Vishnu Nayak
authors.initials: VN
authors.lastname: Badavath
authors.affiliation: Department of Biochemistry, Faculty of Pharmacy, Hacettepe University , Sıhhiye, 06100, Ankara, Turkey.
authors.forename: İpek
authors.initials: İ
authors.lastname: Baysal
authors.affiliation: Department of Biochemistry, Faculty of Pharmacy, Hacettepe University , Sıhhiye, 06100, Ankara, Turkey.
authors.forename: Gulberk
authors.initials: G
authors.lastname: Ucar
authors.affiliation: Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology , Mesra, Ranchi, Jharkhand 835 215, India.
authors.forename: Barij Nayan
authors.initials: BN
authors.lastname: Sinha
authors.affiliation: Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology , Mesra, Ranchi, Jharkhand 835 215, India.
authors.forename: Venkatesan
authors.initials: V
authors.lastname: Jayaprakash
keywords: Human monoamine oxidase; enzyme inhibitors; molecular docking simulation; pyrazoline
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