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Synthesis of some novel benzoxazolinonylcarboxamides as potential  anti-inflammatory agents  

Posted on 1. July, 2014.

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Nonsteroidal anti-inflammatory drugs (NSAIDs) represent one of the most extensively utilised classes of pharmaceutical agents worldwide, and have been used in the treatment of pain, nociception, fever and inflammatory diseases, especially arthritis.

Since the discovery of an inducible isoform of the enzyme COX later identified as COX-2, in the early 1990s by Needleman, Simmons and Herschman’s group, numerous COX-2 selective inhibitors have been proposed. Several studies show that the inhibition of cyclooxygenases-2 can delay or prevent certain forms of cancer. 
In addition to intensive drug discovery programs targeting COX-2 inhibitors, another and perhaps more original approach has been concerned with the exploration of the pharmacological potentials of 2-amino-4,6-dimethylpyridine amide derivatives as mixed inhibitors of both eicosanoid biosynthesis and IL-1/TNF-alpha production. The major compounds in this family are benzamide or phenylacetamide derivatives of 2-amino-4,6-dimethylpyridine.

In this study, we report the synthesis and characterisation of some novel benzoxazolinonic carboxamide derivatives.

Authors: Liacha Messaoud, Yahia Wassila, Seddiki Khemissi, Adjeroud Yasmina and Chabane Hanane
Laboratoire de Synthèse et Biocatalyse Organique, Faculté des Sciences, Université Badji-Mokhtar-Annaba, PB 12, 23000 Annaba, Algeria

Keywords: carboxamides, 2(3H)-benzoxazolone, Friedel–Crafts, acylation, anti-inflammatory drugs

Read the full article in Journal of Chemical Research, Volume 38, Number 6, June 2014, pp. 331-333.


Image: Preparation of (Benzoxazolinon-6-yl)carboxamides from (Benzoxazolinon-6-yl)carboxylic acids