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Título: | Synthesis and in vitro study of nitro- and methoxy-2-phenylbenzofurans as human monoamine oxidase inhibitors |
Autor: | Delogu, G. L.; Kumar, A.; Gatto, G.; Bustelo, F.; Saavedra, Lucía M. CSIC; Rodríguez-Franco, María Isabel CSIC ORCID ; Laguna, Reyes; Viña, Dolores | Palabras clave: | 2-Phenylbenzofurans Monoamine oxidase inhibitors Docking studies |
Fecha de publicación: | 2021 | Editor: | Academic Press | Citación: | Bioorganic Chemistry 107 (2021) | Resumen: | A new series of 2-phenylbenzofuran derivatives were designed and synthesized to determine relevant structural features for the MAO inhibitory activity and selectivity. Methoxy substituents were introduced in the 2-phenyl ring, whereas the benzofuran moiety was not substituted or substituted at the positions 5 or 7 with a nitro group. Substitution patterns on both the phenyl ring and the benzofuran moiety determine the affinity for MAO-A or MAO-B. The 2-(3-methoxyphenyl)-5-nitrobenzofuran 9 was the most potent MAO-B inhibitor (IC = 0.024 µM) identified in this series, whereas 7-nitro-2-phenylbenzofuran 7 was the most potent MAO-A inhibitor (IC = 0.168 µM), both acting as reversible inhibitors. The number and position of the methoxyl groups on the 2-phenyl ring, have an important influence on the inhibitory activity. Molecular docking studies confirmed the experimental results and highlighted the importance of key residues in enzyme inhibition. | Versión del editor: | http://dx.doi.org/10.1016/j.bioorg.2020.104616 | URI: | http://hdl.handle.net/10261/249636 | DOI: | 10.1016/j.bioorg.2020.104616 | Identificadores: | doi: 10.1016/j.bioorg.2020.104616 issn: 1090-2120 |
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