Abstract
The carboxamide derivatives of Febuxostat were synthesized via the reaction of Febuxostat with various amines through by Schotten-Baumann reaction. All the synthesized compounds have been evaluated for their in vitro Xanthine Oxidase inhibitory activity. The present study reveals that most of carboxamides were acting as better XO inhibitors and play an important role in decreasing uricacid levels. Almost all the compounds surprisingly showed nearly 30% higher XO inhibition activities than the standard Allopurinol. 3h, 3k and 3l stand as the best among the synthesized compounds.
Keywords: Febuxostat carboxamide derivatives, Schotten-Baumann reaction, Xanthine oxidase (XO) inhibitory activity.
Letters in Drug Design & Discovery
Title:Augmenting the Xanthine Oxidase Inhibitory Activity of Febuxostat by its Structural Modification
Volume: 11 Issue: 2
Author(s): Kuruva Chandra Sekhar, Golla Madhava, Katla Venkata Ramana, CH. Rama Murthy and Chamarthi Naga Raju
Affiliation:
Keywords: Febuxostat carboxamide derivatives, Schotten-Baumann reaction, Xanthine oxidase (XO) inhibitory activity.
Abstract: The carboxamide derivatives of Febuxostat were synthesized via the reaction of Febuxostat with various amines through by Schotten-Baumann reaction. All the synthesized compounds have been evaluated for their in vitro Xanthine Oxidase inhibitory activity. The present study reveals that most of carboxamides were acting as better XO inhibitors and play an important role in decreasing uricacid levels. Almost all the compounds surprisingly showed nearly 30% higher XO inhibition activities than the standard Allopurinol. 3h, 3k and 3l stand as the best among the synthesized compounds.
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Chandra Sekhar Kuruva, Madhava Golla, Venkata Ramana Katla, Rama Murthy CH. and Naga Raju Chamarthi, Augmenting the Xanthine Oxidase Inhibitory Activity of Febuxostat by its Structural Modification, Letters in Drug Design & Discovery 2014; 11 (2) . https://dx.doi.org/10.2174/15701808113109990056
DOI https://dx.doi.org/10.2174/15701808113109990056 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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