6 documents found, page 1 of 1
Rivastigmine-Benzimidazole Hybrids as Promising Multitarget Metal-Modulating Co...
Vicente-Zurdo, David; Brunetti, Leonardo; Piemontese, Luca; Guedes, Beatriz; Cardoso, Sandra M.; Chavarria, Daniel; Borges, Fernanda; Madrid, YolandaWith the goal of combating the multi-faceted Alzheimer's disease (AD), a series of Rivastigmine-Benzimidazole (RIV-BIM) hybrids was recently reported by us as multitarget-directed ligands, thanks to their capacity to tackle important hallmarks of AD. In particular, they exhibited antioxidant activity, acted as cholinesterase inhibitors, and inhibited amyloid-β (Aβ) aggregation. Herein, we moved forward in this ...
Novel Donepezil-Arylsulfonamide Hybrids as Multitarget-Directed Ligands for Pot...
Queda, Fausto; Calò, Sonia; Gwizdala, Karolina; Magalhães, João D.; Cardoso, Sandra M.; Chaves, Sílvia; Piemontese, Luca; Santos, M. AméliaAlzheimer's disease (AD) is one of the most devastating neurodegenerative disorders, characterized by multiple pathological features. Therefore, multi-target drug discovery has been one of the most active fields searching for new effective anti-AD therapies. Herein, a series of hybrid compounds are reported which were designed and developed by combining an aryl-sulfonamide function with a benzyl-piperidine moie...
Derivatives of Tenuazonic Acid as Potential New Multi-Target Anti-Alzheimer's D...
Poliseno, Viviana; Chaves, Sílvia; Brunetti, Leonardo; Loiodice, Fulvio; Carrieri, Antonio; Laghezza, Antonio; Tortorella, Paolo; Magalhães, João D.Alzheimer's disease (AD) is generally recognized as a multifactorial neurodegenerative pathology with an increasing impact on society. Tenuazonic acid (TA) is a natural compound that was recently identified as a potential multitarget ligand with anti-cholinesterase, anti-amyloidogenic and antioxidant activities. Using its structure as a chemical scaffold, we synthesized and evaluated new derivatives (1-5), incl...
Novel tacrine-benzofuran hybrids as potential multi-target drug candidates for ...
Fancellu, Gaia; Chand, Karam; Tomás, Daniel; Orlandini, Elisabetta; Piemontese, Luca; Silva, Diana F.; Cardoso, Sandra M.; Chaves, SílviaPursuing the widespread interest on multi-target drugs to combat Alzheimer´s disease (AD), a new series of hybrids was designed and developed based on the repositioning of the well-known acetylcholinesterase (AChE) inhibitor, tacrine (TAC), by its coupling to benzofuran (BF) derivatives. The BF framework aims to endow the conjugate molecules with ability for inhibition of AChE (bimodal way) and of amyloid-beta ...
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, VitoA 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. AméliaA 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...