| Autor: |
Anton A. Shetnev, Julia A. Efimova, Mikhail K. Korsakov, Anél Petzer, Jacobus P. Petzer |
| Jazyk: |
angličtina |
| Rok vydání: |
2024 |
| Předmět: |
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| Zdroj: |
Molbank, Vol 2024, Iss 1, p M1787 (2024) |
| Druh dokumentu: |
article |
| ISSN: |
1422-8599 |
| DOI: |
10.3390/M1787 |
| Popis: |
4-(2-Methyloxazol-4-yl)benzenesulfonamide was synthesized by the reaction of 4-(2-bromoacetyl)benzenesulfonamide with an excess of acetamide. The compound was evaluated as a potential inhibitor of human monoamine oxidase (MAO) A and B and was found to inhibit these enzymes with IC50 values of 43.3 and 3.47 μM, respectively. The potential binding orientation and interactions of the inhibitor with MAO-B were examined by molecular docking, and it was found that the sulfonamide group binds and interacts with residues of the substrate cavity. 4-(2-Methyloxazol-4-yl)benzenesulfonamide showed no cytotoxic effect against human stromal bone cell line (HS-5) in the concentration range of 1–100 µmol. Thus, the new selective MAO-B inhibitor was identified, which may be used as the lead compound for the development of antiparkinsonian agents. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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