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MELETLİ, FURKAN

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MELETLİ

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Author: DEMİR, SERAP × Subject: Biochemistry ×

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    Design, synthesis and biological evaluation of novel benzocoumarin derivatives as potent inhibitors of MAO-B activity
    (2024-11-15) MELETLİ, FURKAN; DEMİR, SERAP; DANIŞ, ÖZKAN; MELETLİ F., Gündüz C., Alparslan M. M., ATTAR A., DEMİR S., İskit E., DANIŞ Ö.
    The continued research of novel reversible inhibitors targeting monoamine oxidase (MAO) B remains crucial for effectively symptomatic treatment of Parkinson\"s disease. In this study we synthesized and evaluated a new series of 3-aryl benzo[g] and benzo[h] coumarin derivatives as MAO-B inhibitors. Compound A6 has been found to display the most potent inhibitory activity and selectivity against the MAO-B isoform (IC50 = 13 nM and SI = >7693.31 respectively). Inhibition mode of A6 on MAO-B was predicted as mixed reversible inhibition with a Ki value of 3.274 nM. Furthermore, in order to elaborate structure–activity relationships, the binding mode of A6 was investigated by molecular docking simulations.