English
español
Please use this identifier to cite or link to this item:
http://hdl.handle.net/10261/110035
Share/Impact:
Statistics |
![]() ![]() ![]() |
|
|
Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL | DATACITE | |||
|
Title: | Potent and selective MAO-B inhibitory activity: Amino- versus nitro-3-arylcoumarin derivatives |
Authors: | Matos, M. J.; Rodríguez-Enríquez, F.; Vilar, S.; Santana, Lourdes; Uriarte, E.; Hripcsak, G.; Estrada, Martín ![]() ![]() |
Keywords: | 3-Arylcoumarins Perkin reaction Monoamine oxidase inhibitors PAMPA assay ADME theoretical properties Docking studies |
Issue Date: | 2015 |
Publisher: | Elsevier |
Citation: | Bioorganic and Medicinal Chemistry Letters 25: 642-648 (2015) |
Abstract: | In 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. |
URI: | http://hdl.handle.net/10261/110035 |
DOI: | 10.1016/j.bmcl.2014.12.001 |
Identifiers: | doi: 10.1016/j.bmcl.2014.12.001 issn: 0960-894X e-issn: 1464-3405 |
Appears in Collections: | (IQM) Artículos |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
accesoRestringido.pdf | 15,38 kB | Adobe PDF | ![]() View/Open | |
Publ 66 (Potent and selective MAO-B inhibitory activity).pdf | 387,01 kB | Adobe PDF | ![]() View/Open |
Show full item record
Review this work
Review this work
Related articles:
WARNING: Items in Digital.CSIC are protected by copyright, with all rights reserved, unless otherwise indicated.