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.
- Full Text:
PDF
- DOI:10.5539/ijc.v8n1p49
Journal Metrics
h-index (December 2022): 32
i10-index (December 2022): 145
h5-index (December 2022): N/A
h5-median(December 2022): N/A
( The data was calculated based on Google Scholar Citations. Click Here to Learn More. )
Index
- Academic Journals Database
- Bibliography and Index of Geology
- CAB Abstracts
- CAS (American Chemical Society)
- COPAC
- Elektronische Zeitschriftenbibliothek (EZB)
- EuroPub Database
- Excellence in Research for Australia (ERA)
- Genamics JournalSeek
- Google Scholar
- Infotrieve
- Mendeley
- MIAR
- RePEc
- ResearchGate
- ROAD
- SHERPA/RoMEO
Contact
- Albert JohnEditorial Assistant
- ijc@ccsenet.org