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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

Synthesis and Anti-Oxidant Evaluation of Some Novel Sulfa Drugs

Author(s): Moustafa A. Gouda* and Belal H.M. Hussein

Volume 14, Issue 12, 2017

Page: [1425 - 1432] Pages: 8

DOI: 10.2174/1570180814666170607144811

Price: $65


Background: Curcumins were reported to possess anti-inflammatory and antiangiogenic. Furthermore, Curcumin is a very potent free radical scavenger than vitamin E. Moreover, cyanoacetamides were reported to possess, antimicrobial antifungal, insulin releasing, antiinflammatory and antitumor. Thus the present study focuses on the synthesis of some novel structure hybrids incorporating either curcumin or cyanoacetamide with sulphonamide, aiming to reach a more potent antioxidant agent.

Methods: 4-arylazoenol derivatives 12-16 and E-hydrazo derivatives 19-23 were prepared and their structure was confirmed by variable spectra analysis. The newly synthesized compounds were screened for their antioxidant activity using ABTS and Bleomycin-dependent DNA damage methods.

Results: Coupling of the diazonium salts 7-11 of different sulpha drugs with curcumin 1 or with cyanoacetamide 18 afforded the corresponding 4-arylazoenol derivatives 12-16 and E-hydrazo derivatives 19-23. Among all the synthesized compounds, 12-16, 18, 20 and 22 were the most potent antioxidant compounds.

Conclusion: The objective of the present study was to synthesize and evaluate the antioxidant activity of some novel sulfonamides structure hybrids incorporating either curcumin or N-[4- (aminosulfonyl) phenyl]-2-cyanoacetamide moiety with the hope of discovering new structure serving as antioxidant agent. The data showed clearly that most of compounds displayed good in vitro antioxidant activities.

Keywords: N-[4-(aminosulfonyl)phenyl]-2-cyanoacetamide, sulphonamides, diazonium salt, anti-oxidant, curcumin, antifungal.

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