| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 7802610 | European Journal of Medicinal Chemistry | 2012 | 14 Pages |
Abstract
⺠The synthesis, pharmacology and molecular modeling of tacrine analogs 21-30 are described. ⺠Tacrine 25 [IC50 (hAChE) = 0.33 ± 0.04 μM] is a mixed type inhibitor (Ki = 81 nM). ⺠Tacrine 25 shows good antioxidant profile (ORAC experiment: 1.47 ± 0.10 Trolox equiv). ⺠Inhibitors 26-28 and 30 are permeable, neuroprotective and less toxic than tacrine. ⺠These tacrine analogs are attractive multipotent therapeutic molecules for AD.
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![Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease](/preview/png/7802610.png "First Page Preview: Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease")
Authors
Emna Maalej, Fakher Chabchoub, MarÃa Jesús Oset-Gasque, Mario Esquivias-Pérez, MarÃa P. González, Leticia Monjas, Concepción Pérez, Cristóbal de los RÃos, MarÃa Isabel RodrÃguez-Franco, Isabel Iriepa, Ignacio Moraleda, Mourad Chioua,