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Design, Synthesis, and In Vitro Evaluation of Hydroxybenzimidazole-Donepezil An...

Chaves, Sílvia; Resta, Simonetta; Rinaldo, Federica; Costa, Marina; Josselin, Romane; Gwizdala, Karolina; Piemontese, Luca; Capriati, Vito

A series of multi-target-directed ligands (MTDLs), obtained by attachment of a hydroxyphenylbenzimidazole (BIM) unit to donepezil (DNP) active mimetic moiety (benzyl-piperidine/-piperazine) was designed, synthesized, and evaluated as potential anti-Alzheimer's disease (AD) drugs in terms of biological activity (inhibition of acetylcholinesterase (AChE) and β-amyloid (Aβ) aggregation), metal chelation, and neuro...


Donepezil structure-based hybrids as potential multifunctional anti-Alzheimer's...

Piemontese, Luca; Tomás, Daniel; Hiremathad, Asha; Capriati, Vito; Candeias, Emanuel; Cardoso, Sandra M.; Chaves, Sílvia; Santos, M. Amélia

A new series of multifunctional hybrids, based on the structure of the donepezil (DNP) drug, have been developed and evaluated as potential anti Alzheimer's disease (AD) agents. The rationale of this study was the conjugation of a benzylpiperidine/benzylpiperazine moiety with derivatives of bioactive heterocyclics (benzimidazole or benzofuran), to mimic the main structure of DNP and to endow the hybrids with ad...


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