Donepezil plus chromone plus melatonin hybrids as promising agents for Alzheimer's disease therapy
| Affiliation auteurs | !!!! Error affiliation !!!! |
| Titre | Donepezil plus chromone plus melatonin hybrids as promising agents for Alzheimer's disease therapy |
| Type de publication | Journal Article |
| Year of Publication | 2019 |
| Auteurs | Pachon-Angona I, Refouvelet B, Andrys R, Martin H, Luzet V, Iriepa I, Moraleda I, Diez-Iriepa D, Oset-Gasque M-J, Marco-Contelles J, Musilek K, Ismaili L |
| Journal | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY |
| Volume | 34 |
| Pagination | 479-489 |
| Date Published | JAN 1 |
| Type of Article | Article |
| ISSN | 1475-6366 |
| Mots-clés | Antioxidant, cholinesterases, donepezil, MAO-A, MAO-B, ORAC, Ugi-4MCR |
| Résumé | We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC50 = 11.90 +/- 0.05 nM), moderate hAChE (IC50 = 1.73 +/- 0.34 mu M), hMAO A (IC50 = 2.78 +/- 0.12 mu M), and MAO B (IC50 = 21.29 +/- 3.85 mu M) inhibition, while keeping a strong antioxidant power (3.04 TE, ORAC test). Consequently, the results reported here support the development of new multitarget Donepezil + Chromone + Melatonin hybrids, such as compound 14n, as a potential drug for AD patients cure. [GRAPHICS] . |
| DOI | 10.1080/14756366.2018.1545766 |