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Synthesis and biological evaluation of 4-styrylcoumarin derivatives as inhibitors of TNF-α and IL-6 with anti-tubercular activity

Upadhyay, Kuldip, Bavishi, Abhay, Thakrar, Shailesh, Radadiya, Ashish, Vala, Hardevsinh, Parekh, Shrey, Bhavsar, Dhairya, Savant, Mahesh, Parmar, Manisha, Adlakha, Priti and Shah, Anamik 2011. Synthesis and biological evaluation of 4-styrylcoumarin derivatives as inhibitors of TNF-α and IL-6 with anti-tubercular activity. Biorganic and Medicinal Chemistry Letters 21 (8) , pp. 2547-2549. 10.1016/j.bmcl.2011.02.016

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Abstract

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 1H 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 <6.25 μM.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Publisher: Elsevier
ISSN: 0960-894X
Date of Acceptance: 4 February 2011
Last Modified: 23 Mar 2018 11:08
URI: http://orca-mwe.cf.ac.uk/id/eprint/109870

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