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 ORCID: https://orcid.org/0000-0001-7348-1755, 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 Oct 2022 13:10
URI:	https://orca.cardiff.ac.uk/id/eprint/109870

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