New multifunctional agents and their inhibitory effects on the acetyl cholinesterase enzyme
| Autor: | Murat Gümüş, Ali Dişli, Fatma Arslan, Nurşen Sarı, Kübra Önal |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
chemistry.chemical_classification
010405 organic chemistry Aché General Chemical Engineering Substituent Thio lcsh:TP155-156 General Chemistry Inhibitory postsynaptic potential alzheimer's disease tetrazole inhibition 01 natural sciences Medicinal chemistry language.human_language 0104 chemical sciences lcsh:Biochemistry 010404 medicinal & biomolecular chemistry chemistry.chemical_compound Enzyme chemistry Pyridine language Sodium azide Tetrazole lcsh:QD415-436 lcsh:Chemical engineering |
| Zdroj: | Macedonian Journal of Chemistry and Chemical Engineering, Vol 37, Iss 1, Pp 21-34 (2018) |
| ISSN: | 1857-5625 1857-5552 |
| Popis: | A novel series of 2-((-1-substituted phenyl-1 H -tetrazol-5-yl)thio)-2,3-dihydro-1 H -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-1 H -tetrazol-5-thiol compounds. Then, novel 2-((-1-substituted phenyl-1 H -tetrazol-5-yl)thio)-2,3-dihydro-1 H -inden-1-one compounds were synthesized by treatment of 2,3-dihydro-1 H -inden-1-one with the 1-substituted phenyl-1 H -tetrazol-5-thiol in the presence of I 2 . 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 IC 50 value of 1.75 μM. For the studied compunds all IC 50 values for AChE were in the micromolar range. |
| Databáze: | OpenAIRE |
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