Facile synthesis and docking studies of 7-hydroxyflavanone isoxazoles and acrylates as potential anti-microbial agents
| Autor: | B. Kesava Rao, G. Narasimha, B. China Raju, Y. Jayavardhana Rao, P. Asha Bhanu |
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| Rok vydání: | 2019 |
| Předmět: |
biology
010405 organic chemistry Chemistry Stereochemistry In silico Organic Chemistry Anti-Microbial Agents Biological activity 01 natural sciences DNA gyrase 7-hydroxyflavanone Sterol 0104 chemical sciences 010404 medicinal & biomolecular chemistry Docking (molecular) biology.protein Demethylase General Pharmacology Toxicology and Pharmaceutics |
| Zdroj: | Medicinal Chemistry Research. 29:217-228 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-019-02476-5 |
| Popis: | The present study is aimed to synthesize the novel 7-hydroxyflavanone derived compounds and to assess their biological activity. Two series of compounds such as 2-phenyl-7-((3-phenylisoxazol-5-yl)methoxy)chroman-4-ones (6a–h) and 4-oxo-2-phenylchroman-7-yl acrylates (8a–k) were synthesized from 7-hydroxyflavanone. All the compounds were subjected to anti-microbial activity and molecular docking studies. The results showed that the compounds 6e, 6g–h, 8h–i and 8k were exhibited most potent anti-microbial activity when compared with the standard drugs. Further, the docking studies revealed that the compounds 6a and 8h have the highest binding affinity score of sterol 14-α demethylase and DNA gyrase B respectively. This is the first report assigning unique synthesis of 7-hydroxyflavanone derivatives and their anti-microbial activity proved with in silico studies. Furthermore, the present study is useful for constructive research to synthesize novel compounds along with their biological activity. |
| Databáze: | OpenAIRE |
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