Article
Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase
Author/s | Evangelista, Tereza Cristina Santos
López López, Óscar Ferreira, Sabrina Baptista Fernández-Bolaños Guzmán, José María Sydnes, Magne O. Lindbäck, Emil |
Department | Universidad de Sevilla. Departamento de Electrónica y Electromagnetismo |
Publication Date | 2021 |
Deposit Date | 2022-04-07 |
Published in |
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Abstract | The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers of variable lengths is described. The multivalent inhibition potencies for the tacrine clusters ... The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers of variable lengths is described. The multivalent inhibition potencies for the tacrine clusters were investigated for the inhibition of acetylcholinesterase. Two of the tacrine clusters displayed a small but significant multivalent inhibition potency in which the binding affinity of each of the tacrine binding units increased up to 3.2 times when they are connected to the central scaffold. |
Funding agencies | Junta de Andalucía Universidad de Stavanger. Noruega Ministerio de Ciencia e Innovación (MICIN). España European Commission (EC). Fondo Europeo de Desarrollo Regional (FEDER) |
Project ID. | FQM134
CTQ2016-78703-P |
Citation | Evangelista, T.C.S., López López, Ó., Ferreira, S.B., Fernández-Bolaños Guzmán, J.M., Sydnes, M.O. y Lindbäck, E. (2021). Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase. Journal of Enzyme Inhibition and Medicinal Chemistry, 36 (1), 1659-1664. |
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