Mannich-Benzimidazole Derivatives as Antioxidant and Anticholinesterase Inhibitors: Synthesis, Biological Evaluations, and Molecular Docking Study.

Autor: Alpan AS; Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ege University, Bornova, Izmir, Turkey., Sarıkaya G; Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ege University, Bornova, Izmir, Turkey., Çoban G; Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ege University, Bornova, Izmir, Turkey., Parlar S; Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ege University, Bornova, Izmir, Turkey., Armagan G; Faculty of Pharmacy, Department of Biochemistry, Ege University, Bornova, Izmir, Turkey., Alptüzün V; Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ege University, Bornova, Izmir, Turkey.
Jazyk: angličtina
Zdroj: Archiv der Pharmazie [Arch Pharm (Weinheim)] 2017 Jul; Vol. 350 (7). Date of Electronic Publication: 2017 Apr 05.
DOI: 10.1002/ardp.201600351
Abstrakt: A series of Mannich bases of benzimidazole derivatives having a phenolic group were designed to assess their anticholinesterase and antioxidant activities. The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities were evaluated in vitro by using Ellman's method. According to the activity results, all of the compounds exhibited moderate to good AChE inhibitory activity (except for 2a), with IC 50 values ranging from 0.93 to 10.85 μM, and generally displayed moderate BuChE inhibitory activity. Also, most of the compounds were selective against BuChE. Compound 4b was the most active molecule on the AChE enzyme and also selective. In addition, we investigated the antioxidant effects of the synthesized compounds against FeCl 2 /ascorbic acid-induced oxidative stress in the rat brain in vitro, and the activity results showed that most of the compounds are effective as radical scavengers. Molecular docking studies and molecular dynamics simulations were also carried out.
(© 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
Databáze: MEDLINE
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