Int. J. Mol. Sci. 2014, 15(3), 5115-5127; doi:10.3390/ijms15035115
Article

Synthesis and Biological Evaluation of 2-Aminobenzamide Derivatives as Antimicrobial Agents: Opening/Closing Pharmacophore Site

1,* email, 1email, 1,2email, 1email, 3email, 4email, 5email and 6email
Received: 11 December 2013; in revised form: 28 February 2014 / Accepted: 5 March 2014 / Published: 21 March 2014
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: A series of new 2-aminobenzamide derivatives (110) has been synthesized in good to excellent yields by adopting both conventional and/or a time-efficient microwave assisted methodologies starting from isatoic anhydride (ISA) and characterized on the basis of their physical, spectral and microanalytical data. Selected compounds of this series were then tested against various bacterial (Bacillus subtilis (RCMB 000107) and Staphylococcus aureus (RCMB 000106). Pseudomonas aeruginosa (RCMB 000102) and Escherichia coli (RCMB 000103) and fungal strains (Saccharomyces cerevisiae (RCMB 006002), Aspergillus fumigatus (RCMB 002003) and Candida albicans (RCMB 005002) to explore their potential as antimicrobial agents. Compound 5 was found to be the most active compound among those tested, which showed excellent antifungal activity against Aspergillus fumigatus (RCMB 002003) more potent than standard Clotrimazole, and moderate to good antibacterial and antifungal activity against most of the other strains of bacteria and fungi. Furthermore, potential pharmacophore sites were identified and their activity was related with the structures in the solution.
Keywords: isatoic anhydride; conventional method; microwave method; 2-aminobenzamide; antimicrobial activity
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MDPI and ACS Style

Mabkhot, Y.N.; Al-Majid, A.M.; Barakat, A.; Al-Showiman, S.S.; Al-Har, M.S.; Radi, S.; Naseer, M.M.; Hadda, T.B. Synthesis and Biological Evaluation of 2-Aminobenzamide Derivatives as Antimicrobial Agents: Opening/Closing Pharmacophore Site. Int. J. Mol. Sci. 2014, 15, 5115-5127.

AMA Style

Mabkhot YN, Al-Majid AM, Barakat A, Al-Showiman SS, Al-Har MS, Radi S, Naseer MM, Hadda TB. Synthesis and Biological Evaluation of 2-Aminobenzamide Derivatives as Antimicrobial Agents: Opening/Closing Pharmacophore Site. International Journal of Molecular Sciences. 2014; 15(3):5115-5127.

Chicago/Turabian Style

Mabkhot, Yahia N.; Al-Majid, Abdullah M.; Barakat, Assem; Al-Showiman, Salim S.; Al-Har, Munirah S.; Radi, Smaail; Naseer, Muhammad M.; Hadda, Taibi B. 2014. "Synthesis and Biological Evaluation of 2-Aminobenzamide Derivatives as Antimicrobial Agents: Opening/Closing Pharmacophore Site." Int. J. Mol. Sci. 15, no. 3: 5115-5127.

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