Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines
| Autor: | Bünyamin Özgeriş, Ali Naderi, Süleyman Göksu, İlhami Gülçin, Kadir Aksu, Parham Taslimi |
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| Rok vydání: | 2016 |
| Předmět: |
Antioxidant
biology 010405 organic chemistry Aché medicine.medical_treatment Pharmaceutical Science Phenethylamines 01 natural sciences Acetylcholinesterase Chloride language.human_language 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry.chemical_compound chemistry Carbonic anhydrase Drug Discovery medicine language biology.protein Urea Organic chemistry Butyrylcholinesterase medicine.drug |
| Zdroj: | Archiv der Pharmazie. 349:944-954 |
| ISSN: | 0365-6233 |
| DOI: | 10.1002/ardp.201600183 |
| Popis: | A series of ureas derived from phenethylamines were synthesized and evaluated for human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activities and antioxidant properties. The ureas were synthesized from the reactions of substituted phenethylamines with N,N-dimethylcarbamoyl chloride; then, the synthesized compounds were converted to their corresponding phenolic derivatives via O-demethylation. hCA I and II were effectively inhibited by the newly synthesized compounds, with Ki values in the range of 0.307-0.432 nM for hCA I and 0.149-0.278 nM for hCA II. On the other hand, the Ki parameters of these compounds for AChE and BChE were determined in the range of 0.129-0.434 and 0.095-0.207 nM, respectively. Phenolic ureas also showed good antioxidant activities. |
| Databáze: | OpenAIRE |
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