Dual inhibition of AChE and BuChE by coumarin–benzothiazole hybrids: potent candidates unveiled through innovative screening and docking studies

= 0.9983-0.9992), precision (CV ≤ 7.8%), and accuracy within accepted validation limits. Biological evaluation revealed highly potent inhibitors, particularly 13a and 13m, which exhibited IC₅₀ values of 1.0 ± 0.1 nM and 0.6 ± 0.1 nM against AChE, respectively, compared with 64.9 ± 16.0 nM for donepezil. For BuChE, 13m showed an IC₅₀ of 109.2 ± 14.7 nM, while 13a displayed 1212.5 ± 144.0 nM, both lower than donepezil (2202 ± 326 nM). Kinetic studies confirmed a competitive mechanism of inhibition, with Kᵢ values as low as 0.12 ± 0.02 nM for AChE and 47.76 ± 15.14 nM for BuChE (13m). Molecular docking studies supported these findings, demonstrating key interactions within the catalytic sites of both enzymes. Additionally, in silico evaluations indicated that these derivatives have favorable druglikeness. Together, the results highlight coumarin-benzothiazole derivatives as promising dual-target ChEIs and establish the developed analytical method as a versatile tool for the discovery and characterization of new anti-AD candidates.

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Publication Details

Journal
Bioorganic Chemistry
Published
2026-04-06
DOI
https://doi.org/10.1016/j.bioorg.2026.109838
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
0.00

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article

Dual inhibition of AChE and BuChE by coumarin–benzothiazole hybrids: potent candidates unveiled through innovative screening and docking studies

Fernanda P. Pauli, Marcela Cristina de Moraes, Mayra S. Coutinho, Raissa Alves da Conceição et al.
Bioorganic Chemistry
Synthesis and biological activity
article

Dual inhibition of AChE and BuChE by coumarin–benzothiazole hybrids: potent candidates unveiled through innovative screening and docking studies

Fernanda P. Pauli, Marcela Cristina de Moraes, Mayra S. Coutinho, Raissa Alves da Conceição, Fernando de C. da Silva., Luana da SM Forezi, Evelyn Santana Bezerra, Adriane Amaral, Pamella C.O. de Oliveira, Raíssa G. Gouvea, Lucas G. Amaral, Alessandra M. Teles de Souza
article en

Abstract

= 0.9983-0.9992), precision (CV ≤ 7.8%), and accuracy within accepted validation limits. Biological evaluation revealed highly potent inhibitors, particularly 13a and 13m, which exhibited IC₅₀ values of 1.0 ± 0.1 nM and 0.6 ± 0.1 nM against AChE, respectively, compared with 64.9 ± 16.0 nM for donepezil. For BuChE, 13m showed an IC₅₀ of 109.2 ± 14.7 nM, while 13a displayed 1212.5 ± 144.0 nM, both lower than donepezil (2202 ± 326 nM). Kinetic studies confirmed a competitive mechanism of inhibition, with Kᵢ values as low as 0.12 ± 0.02 nM for AChE and 47.76 ± 15.14 nM for BuChE (13m). Molecular docking studies supported these findings, demonstrating key interactions within the catalytic sites of both enzymes. Additionally, in silico evaluations indicated that these derivatives have favorable druglikeness. Together, the results highlight coumarin-benzothiazole derivatives as promising dual-target ChEIs and establish the developed analytical method as a versatile tool for the discovery and characterization of new anti-AD candidates.

Bioorganic ChemistryVol. 176
Universidade Federal do Rio de Janeiro (BR), Universidade Federal Fluminense (BR), Instituto Federal do Paraná (BR), Universidade do Estado do Rio de Janeiro (BR)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Conselho Nacional de Desenvolvimento Científico e Tecnológico, Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro, Fundação Oswaldo Cruz
Openalex Percentile: Top 29%
Synthesis and biological activity
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