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Synthesis and biological assessment of racemic benzochromenopyrimidinimines as antioxidant, cholinesterase, and $▫ [Aß1-42]▫$ aggregation Inhibitors for Alzheimer's disease therapyDgachi, Youssef ...Given the complex nature of Alzheimer's disease (AD), compounds that are able to simultaneously address two or more AD-associated targets show greater promise for development into drugs for AD ... therapy. Herein we report an efficient two-step synthesis and biological evaluation of new racemic benzochromene derivatives as antioxidants, inhibitors of cholinesterase and ß-amyloid (Aß 41) aggregation. Based on the results of the primary screening, we identified 15-(3-methoxyphenyl)-9,11,12,15-tetrahydro-10H,14H-benzo[5,6]chromeno[2,3-d]pyrido[1,2-a]pyrimidin-14-imine (3e) and 16-(3-methoxyphenyl)-9,10,11,12,13,16-hexahydro-15H-benzo[5,6]chromeno[2,3, 4]pyrimido[1,2-a]azepin-15-imine (3f) as new potential multitarget-directed ligands for AD therapy. Further in-depth biological analysis showed that compound 3f is a good human acetylcholinesterase inhibitor [IC50=(0.36-0.02)microm], has strong antioxidant activity (3.61micromol Trolox equivalents), and moderate Aß41-42 antiaggregating power (40.3%).Source: ChemMedChem : Chemistry Enabling Drug Discovery. - ISSN 1860-7179 (Vol. 11, iss. 12, 2016, str. 1318-1327)Type of material - e-articlePublish date - 2016Language - englishCOBISS.SI-ID - 4022897
Link(s):
http://onlinelibrary.wiley.com/doi/10.1002/cmdc.201500539/abstractSpletna stran dostopna samo z geslom
DOI
Author
Dgachi, Youssef |
Ismaili, Lhassane |
Knez, Damijan, farmacevt |
Benchekroun, Mohamed |
Martin, Hélène, pharmacist |
Szałaj, Natalia |
Wehle, Sarah |
Bautista-Aguilera, Oscar M. |
Luzet, Vincent |
Bonnet, Alexandre |
Malawska, Barbara |
Gobec, Stanislav, 1970- |
Chioua, Mourad |
Drecker, Michael |
Chabchoub, Fakher |
Marco-Contelles, José
Topics
Alzheimerjeva bolezen |
inhibitorji |
antioksidanti |
molekularno modeliranje |
multitarčni ligandi
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Dgachi, Youssef | |
Ismaili, Lhassane | |
Knez, Damijan, farmacevt | 36438 |
Benchekroun, Mohamed | |
Martin, Hélène, pharmacist | |
Szałaj, Natalia | |
Wehle, Sarah | |
Bautista-Aguilera, Oscar M. | |
Luzet, Vincent | |
Bonnet, Alexandre | |
Malawska, Barbara | |
Gobec, Stanislav, 1970- | 15284 |
Chioua, Mourad | |
Drecker, Michael | |
Chabchoub, Fakher | |
Marco-Contelles, José |
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