Synthesis, Biological Assessment and Molecular Modeling of Racemic QuinoPyranoTacrines for Alzheimer's Disease Therapy
| Affiliation auteurs | !!!! Error affiliation !!!! |
| Titre | Synthesis, Biological Assessment and Molecular Modeling of Racemic QuinoPyranoTacrines for Alzheimer's Disease Therapy |
| Type de publication | Journal Article |
| Year of Publication | 2018 |
| Auteurs | Chioua M, Serrano E, Dgachi Y, Martin H, Jun D, Janockova J, Sepsova V, Soukup O, Moraleda I, Chabchoub F, Ismaili L, Iriepa I, Marco-Contelles J |
| Journal | CHEMISTRYSELECT |
| Volume | 3 |
| Pagination | 461-466 |
| Date Published | JAN 17 |
| Type of Article | Article |
| ISSN | 2365-6549 |
| Mots-clés | Alzheimer's disease, Biological Evaluation, Molecular modeling, QuinoPyranoTacrines, synthesis |
| Résumé | In this report we describe the synthesis, biological evaluation and molecular modeling of new tacrine analogues such as QuinoPyranTacrines (QPTs), designed by juxtaposition of 1,4-naphthoquinone and tacrine. From these results we have identified QPT16 as a permeable, selective human acetylcholinesterase inhibitor [IC50= 1.1 +/- 0.15 mu M], 3.5-fold less-hepatotoxic than tacrine at 1000 mu M concentration, and consequently, a potential new hit-compound for further investigation targeted to find a new agent for AD therapy. |
| DOI | 10.1002/slct.201702781 |