Design, synthesis, molecular docking and biological evaluation of β-carboline derivatives as cholinesterase inhibitors

Baréa, Paula; Yamazaki, Diego Alberto dos Santos; Lima, Diego de Souza; Seixas, Flávio Augusto Vicente; Costa, Willian Ferreira da; Gauze, Gisele F.; Sarragiotto, María Helena

doi:10.1016/j.molstruc.2022.134291

Cited by 1 publication

(1 citation statement)

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“…AChE hydrolyzes the bulk of ACh in the brain under physiologically normal conditions. As a result, the most popular methods for treating AD have focused on raising acetylcholine levels by decreasing the activity of the AChE enzyme [4][5][6][7]. AChE's sister enzyme, BChE, has recently drawn more attention due to a potential connection to Alzheimer's disease [8].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Evaluation of Pyrrol-thiazole Derivatives as AChE and BuChE Inhibitory and Antioxidant Activities

Acar Çevik,

Ercetin

2023

Cumhuriyet Science Journal

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Thiazole rings are one of the most frequently used heterocyclic moieties and are found in a wide variety of biologically active chemicals. In this research project, we report the synthesis and biological activities of some new thiazole derivatives (2a-2c) as potent anti-Alzheimer’s agents. These final compounds’ structures were characterized by spectral (1H NMR, 13C NMR, and MS spectra) analyses. The highest inhibitory activity against AChE was demonstrated by compound 2c (23.73 ± 0.018 %) with chloro substitution at the meta and para positions of the phenyl ring, while the highest inhibitory activity against BuChE was produced by compound 2a (28.87± 0.003 %) with cyano substitution at the f position of the phenyl ring. Ferrous ion-chelating and DPPH techniques were also used to assess the compounds' antioxidant properties. Compound 2a showed antioxidant effect according to the DPPH method with an IC50 value of 27.18 ± 0.009 µM.

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