New multifunctional agents and their inhibitory effects on the acetyl cholinesterase enzyme
-
Published:2018-06-01
Issue:1
Volume:37
Page:21
-
ISSN:1857-5625
-
Container-title:Macedonian Journal of Chemistry and Chemical Engineering
-
language:
-
Short-container-title:Maced. J. Chem. Chem. Eng.
Author:
Dişli Ali,Gümüş Murat,Önal Kübra,Sarı Nurşen,Arslan Fatma
Abstract
A novel series of 2-((-1-substituted phenyl-1H-tetrazol-5-yl)thio)-2,3-dihydro-1H-inden-1-one compounds were designed, synthesized, and evaluated as multi-potent anti-Alzheimer drug candidates. First, treatment of various organic isothiocyanates with sodium azide in the presence of pyridine gave corresponding 1-substituted phenyl-1H-tetrazol-5-thiol compounds. Then, novel 2-((-1-substituted phenyl-1H-tetrazol-5-yl)thio)-2,3-dihydro-1H-inden-1-one compounds were synthesized by treatment of 2,3-dihydro-1H-inden-1-one with the 1-substituted phenyl-1H-tetrazol-5-thiol in the presence of I2. The synthesized compounds were characterized by spectroscopic methods. The inhibitory effects of the synthesized compounds on the acetyl cholinesterase enzyme (AChE) were then tested. An o-iodo substituent displayed higher activity compared to the other analogs. The o-iodo substituent showed a mixed-type of the AChE with an IC50 value of 1.75 μM. For the studied compunds all IC50 values for AChE were in the micromolar range.
Publisher
Society of Chemists and Technologists of Macedonia
Subject
General Chemical Engineering,General Chemistry
Cited by
1 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献