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Synthesis and biological evaluation of 2-aminobenzamide derivatives as antimicrobial agents: opening/closing pharmacophore site.

Abstract：

:A series of new 2-aminobenzamide derivatives (1-10) 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.

journal_name

Int J Mol Sci

journal_title

International journal of molecular sciences

authors

Mabkhot YN,Al-Majid AM,Barakat A,Al-Showiman SS,Al-Har MS,Radi S,Naseer MM,Hadda TB

doi

10.3390/ijms15035115

subject

Has Abstract

pub_date

2014-03-21 00:00:00

pages

5115-27

issue

3

issn

1422-0067

pii

ijms15035115

journal_volume

15

pub_type

杂志文章

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