Synthesis, Biological Evaluation and 2D-QSAR Studies of Novel 6-Oxo-Pyridine-3-Carboxamide Derivatives as Antimicrobial and Antifungal Agents


  •  Hend El-Sehrawi    
  •  Dalia Soliman    
  •  Maha Khalifa    
  •  Omneya El-Bakry    

Abstract

In this study twenty six novel derivatives of 6-oxo-pyridine-3-carboxamide were synthesized and evaluated as antibacterial and antifungal agents. Synthesis of the
2-amino-4-methyl-6-oxo-N,1-diphenyl-1,6-dihydropyridine-3-carboxamide 1 was carried out by reacting equimolar quantities of acetoacetanilide and cyanoacetanilide in ethanol using triethylamine as a catalyst. The results of the in vitro antimicrobial evaluation showed that, the
6-oxo-N,1-diphenyl-5-(p-tolyldiazenyl)-1,6-dihydropyridine-3-carboxamide, 5c displayed broad-spectrum antibacterial activity which was equipotent to both Ampicillin and Gentamicin against the tested bacteria. Moreover, compounds 3a, 5c and 9b were equipotent to the reference drug, Amphotericin B, against Aspergillus fumigatus (MIC = 1.95µg/ml). 2D QSAR studies were carried out in order to correlate the observed activity to the binding mode of these compounds, in addition to their molecular properties that might be controlling their activities.



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  • ISSN(Print): 1916-9698
  • ISSN(Online): 1916-9701
  • Started: 2009
  • Frequency: semiannual

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