Synthesis and biological evaluation of 4-styrylcoumarin derivatives as inhibitors of TNF-α and IL-6 with anti-tubercular activity
| Autor: | Manisha Parmar, Kuldip Upadhyay, Shrey Parekh, Priti Adlakha, Hardevsinh Vala, Shailesh Thakrar, Dhairya Bhavsar, Ashish Radadiya, Anamik Shah, Mahesh M. Savant, Abhay Bavishi |
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| Rok vydání: | 2010 |
| Předmět: |
Nitrile
Stereochemistry Clinical Biochemistry Anti-Inflammatory Agents Antitubercular Agents Pharmaceutical Science Microbial Sensitivity Tests Biochemistry Chemical synthesis chemistry.chemical_compound Coumarins Drug Discovery Molecular Biology Antibacterial agent chemistry.chemical_classification Bicyclic molecule Interleukin-6 Tumor Necrosis Factor-alpha Organic Chemistry Mycobacterium tuberculosis In vitro chemistry Proton NMR Molecular Medicine Knoevenagel condensation Lactone |
| Zdroj: | Bioorganicmedicinal chemistry letters. 21(8) |
| ISSN: | 1464-3405 |
| Popis: | A series of 4-styrylcoumarin have been synthesized by Knoevenagel condensation between substituted 4-methylcoumarin-3-carbonitrile and different heterocyclic or aromatic aldehydes. 4-Methylcoumarin-3-carbonitrile has been synthesized by the base catalyzed reaction between substituted 2-hydroxyacetophenone and ethyl cyanoacetate. The structures of the newly synthesized compounds were confirmed by (1)H NMR, IR and mass spectral analysis. All the compounds were evaluated for their anti-inflammatory activity (against TNF-α and IL-6) and anti-tubercular activity. Compounds 6a, 6h and 6j exhibited promising activity against IL-6 with 72-87% inhibition and compound 6v showed potent activity against TNF-α with 73% inhibition at 10 μM concentration. Whereas compounds 6n, 6o, 6r and 6u showed very good anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain at |
| Databáze: | OpenAIRE |
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