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Potent and selective MAO-B inhibitory activity: Amino- versus nitro-3-arylcoumarin derivatives

AuthorsMatos, M. J.; Rodríguez-Enríquez, F.; Vilar, S.; Santana, Lourdes; Uriarte, E.; Hripcsak, G.; Estrada, Martín ; Rodríguez-Franco, María Isabel ; Viña, D.
Perkin reaction
Monoamine oxidase inhibitors
PAMPA assay
ADME theoretical properties
Docking studies
Issue Date2015
CitationBioorganic and Medicinal Chemistry Letters 25: 642-648 (2015)
AbstractIn this study we synthesized and evaluated a new series of amino and nitro 3-arylcoumarins as hMAO-A and hMAO-B inhibitors. Compounds 2, 3, 5 and 6 presented a better activity and selectivity profile against the hMAO-B isoform (IC50 values between 2 and 6 nM) than selegiline. In general, the amino derivatives (4-6) proved to be more selective against MAO-B than the nitro derivatives (1-3). Additionally, a theoretical study of some physicochemical properties, PAMPA and reversibility assays for the most potent derivative, and molecular docking simulations were carried out to further explain the pharmacological results, and to identify the hypothetical binding mode for the compounds inside the hMAO-B.
Identifiersdoi: 10.1016/j.bmcl.2014.12.001
issn: 0960-894X
e-issn: 1464-3405
Appears in Collections:(IQM) Artículos
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