M. Farrag, A., M. Elsehrawi, H., S. Younes, A. (2015). Synthesis, Antimicrobial Evaluation and Docking Study of Novel Heterocyclic Compounds Bearing a Biologically Active Sulfonamide Moiety. test, 1(1), 7-15. doi: 10.12785/jpac/010104
Amel M. Farrag; Hend M. Elsehrawi; Amel S. Younes. "Synthesis, Antimicrobial Evaluation and Docking Study of Novel Heterocyclic Compounds Bearing a Biologically Active Sulfonamide Moiety". test, 1, 1, 2015, 7-15. doi: 10.12785/jpac/010104
M. Farrag, A., M. Elsehrawi, H., S. Younes, A. (2015). 'Synthesis, Antimicrobial Evaluation and Docking Study of Novel Heterocyclic Compounds Bearing a Biologically Active Sulfonamide Moiety', test, 1(1), pp. 7-15. doi: 10.12785/jpac/010104
M. Farrag, A., M. Elsehrawi, H., S. Younes, A. Synthesis, Antimicrobial Evaluation and Docking Study of Novel Heterocyclic Compounds Bearing a Biologically Active Sulfonamide Moiety. test, 2015; 1(1): 7-15. doi: 10.12785/jpac/010104

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Heterocyclic Compounds Bearing a Biologically Active Sulfonamide Moiety

Journal of Pharmaceutical and Applied Chemistry
Volume 1, Issue 1, May 2015, Pages 7-15    PDF (384.49 K)
Document Type: Original Article
DOI: 10.12785/jpac/010104
Authors
Amel M. Farrag1; Hend M. Elsehrawi2; Amel S. Younes2
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al- Azhar University.
2Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al- Azhar University
Abstract
In the present work,we aimed to synthesize and evaluate in vitro antibacterial and antifungal activities of new 
heterocyclic compounds bearing sulfadiazine moiety. Among the synthesized compounds, arylidine (3f) displayed 
significant antibacterial activity against S.pneumoniae (IC50, 22.46µg/mL, comparable to ampicillin IC50 value, 22.76 
µg/mL),whereas, 2-pyridone (4f)showed the highest antifungal activity against G.candidum (IC50,8.63µg/mL, comparable 
to amphotericin B,IC50, 11.63 µg/mL).Its antibacterial activity against S.pneumoniae was (IC50,13.84 µg/mL, comparable to 
ampicillin, IC50, 22.76µg/mL) and E.coli (IC50,29.89 µg/mL, comparable to gentamycin ,IC50,29.42µg/mL) respectively.On 
the other hand 2-imino chromene (5a) displayed significant antibacterial activities against S.pneumoniae (IC50,19.84µg/mL, 
comparable to ampicillin , IC50, 22.76 µg/mL) and exhibited antifungal activity against G.candidum (IC50,12.63 µg/mL, 
comparable to amphotericin B, IC50 , 11.63 µg/mL) respectively.In general,all of the synthesized compounds exhibited 
better antimicrobial activities than sulfadiazine. Molecular docking studies indicated that the newly synthesized compounds 
could occupy both p-aminobenzoic acid (PABA) and pterin binding pockets of the dihydropteroate synthase (DHPS), 
suggesting that the target compounds could act by the inhibition of microbial DHPS enzyme.These derivatives contain 
sulfonamide moiety as well as heterocyclic moiety that increase the lipophilic characters of the synthesized compounds 
hence enhance its absorption.
Keywords
Antimicrobial agents; Molecular docking; Sulfonamide and Pyridone
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