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Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease
We report herein the straightforward two-step synthesis and biological assessment of novel racemic benzochromenopyrimidinones as non-hepatotoxic, acetylcholinesterase inhibitors with antioxidative properties. Among them, compound 3Bb displayed a mixed-type inhibition of human acetylcholinesterase (I...
| Autores principales: | , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2016
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273488/ https://www.ncbi.nlm.nih.gov/pubmed/27187348 http://dx.doi.org/10.3390/molecules21050634 |
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| author | Dgachi, Youssef Bautista-Aguilera, Oscar M. Benchekroun, Mohamed Martin, Hélène Bonet, Alexandre Knez, Damijan Godyń, Justyna Malawska, Barbara Gobec, Stanislav Chioua, Mourad Janockova, Jana Soukup, Ondrej Chabchoub, Fakher Marco-Contelles, José Ismaili, Lhassane |
| author_facet | Dgachi, Youssef Bautista-Aguilera, Oscar M. Benchekroun, Mohamed Martin, Hélène Bonet, Alexandre Knez, Damijan Godyń, Justyna Malawska, Barbara Gobec, Stanislav Chioua, Mourad Janockova, Jana Soukup, Ondrej Chabchoub, Fakher Marco-Contelles, José Ismaili, Lhassane |
| author_sort | Dgachi, Youssef |
| collection | PubMed |
| description | We report herein the straightforward two-step synthesis and biological assessment of novel racemic benzochromenopyrimidinones as non-hepatotoxic, acetylcholinesterase inhibitors with antioxidative properties. Among them, compound 3Bb displayed a mixed-type inhibition of human acetylcholinesterase (IC(50) = 1.28 ± 0.03 μM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line. |
| format | Online Article Text |
| id | pubmed-6273488 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2016 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-62734882018-12-28 Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease Dgachi, Youssef Bautista-Aguilera, Oscar M. Benchekroun, Mohamed Martin, Hélène Bonet, Alexandre Knez, Damijan Godyń, Justyna Malawska, Barbara Gobec, Stanislav Chioua, Mourad Janockova, Jana Soukup, Ondrej Chabchoub, Fakher Marco-Contelles, José Ismaili, Lhassane Molecules Article We report herein the straightforward two-step synthesis and biological assessment of novel racemic benzochromenopyrimidinones as non-hepatotoxic, acetylcholinesterase inhibitors with antioxidative properties. Among them, compound 3Bb displayed a mixed-type inhibition of human acetylcholinesterase (IC(50) = 1.28 ± 0.03 μM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line. MDPI 2016-05-14 /pmc/articles/PMC6273488/ /pubmed/27187348 http://dx.doi.org/10.3390/molecules21050634 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/). |
| spellingShingle | Article Dgachi, Youssef Bautista-Aguilera, Oscar M. Benchekroun, Mohamed Martin, Hélène Bonet, Alexandre Knez, Damijan Godyń, Justyna Malawska, Barbara Gobec, Stanislav Chioua, Mourad Janockova, Jana Soukup, Ondrej Chabchoub, Fakher Marco-Contelles, José Ismaili, Lhassane Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease |
| title | Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease |
| title_full | Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease |
| title_fullStr | Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease |
| title_full_unstemmed | Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease |
| title_short | Synthesis and Biological Evaluation of Benzochromenopyrimidinones as Cholinesterase Inhibitors and Potent Antioxidant, Non-Hepatotoxic Agents for Alzheimer’s Disease |
| title_sort | synthesis and biological evaluation of benzochromenopyrimidinones as cholinesterase inhibitors and potent antioxidant, non-hepatotoxic agents for alzheimer’s disease |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273488/ https://www.ncbi.nlm.nih.gov/pubmed/27187348 http://dx.doi.org/10.3390/molecules21050634 |
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