Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
7802480 | European Journal of Medicinal Chemistry | 2012 | 6 Pages |
Abstract
⺠Pyridonepezils1-8 were designed and synthesized as dual AChEI, binding the CAS and PAS of the enzyme. ⺠The biological evaluation of molecules 1-8 showed that most of these compounds are potent AChEI. ⺠Compound 7, the most potent, is 703-fold more selective for hAChE than for hBuChE. ⺠The ability of compound 7 to interact with the PAS and CAS of AChE was confirmed by molecular modeling. ⺠Inhibitors 2-8 are permeable as determined in the PAMPA-BBB assay.
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Authors
Abdelouahid Samadi, MartÃn Estrada, Concepción Pérez, MarÃa Isabel RodrÃguez-Franco, Isabel Iriepa, Ignacio Moraleda, Mourad Chioua, José Marco-Contelles,