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Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase.

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 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.

SUBMITTER: Evangelista TCS

PROVIDER: S-EPMC8317962 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature

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Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase.

Evangelista Tereza Cristina Santos TCS López Óscar Ó Ferreira Sabrina Baptista SB Fernández-Bolaños José G JG Sydnes Magne O MO Lindbäck Emil E

Journal of enzyme inhibition and medicinal chemistry 20211201 1

The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold <i>via</i> 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 t ...[more]

PMID: 34294013

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