ANTIMICROBIAL ACTIVITY OF PROTON SALTS OF 3-(SULFAMOYLPHENYLCARBAMOYL)ACRYLIC ACID DERIVATIVES WITH AMINOPYRIDINE DERIVATIVES

Abstract

Ten proton transfer salts (9-18) were synthesized from the reaction of 2-aminopyridine (1), 2-amino-3/4/5/6-methylpyridines (2-5) and 3-aminomethylpyridine (6) with (E)-3-(3/4-sulfamoylphenylcarbamoyl)acrylic acid (7 and 8), respectively. Bacillus subtilis (wild culture), Candida albicans (ATCC 14053) (yeast), Enterococcus faecalis (ATCC 29212) (Gram positive), Escherichia coli (ATCC 25922), Listeria monocytogenes (ATCC 7644), Pseudomonas aeruginosa (ATCC 27853), Staphylococcus aureus (NRRL B-767) (Gram negative) bacterial microorganisms have been tested against the antimicrobial evaluation of compounds (1–18). Vancomycin, Cefepime, Levofloxacin and the antifungal substance Fluconazole were used as antibacterial reference compounds for comparing the MIC values of 1-18. Compounds 1, 3-6, 8-13, 15, 17 and 18 for E. faecalis, 5 for B. subtilis, 1, 3-12, 15, 17 and 18 for S. aureus, 3, 9, 10, 13, 15 and 17 for L. monocytogenes, 16 for E. Coli and 4 for P. aeruginosa the best effect are observed. Proton transfer salts {9, 14, 15 and 17} were showed higher effect than Fluconazole while other compounds (except compounds 2 and 4) had similar effects with Fluconazole. The compounds 2 and 4 showed less activity than Fluconazole.

Keywords

• 2-Aminopyridine derivatives
• 3/4-(Sulfamoylphenylcarbamoyl) acrylic acid
• Proton transfer salt
• Antibacterial and antifungal activity

Supporting Institution

Kütahya Dumlupınar Üniversitesi

Project Number

2013/36, 2019/12

Thanks

This work was supported by Kütahya Dumlupınar University Research Foundation (Grant No: 2013/36 and 2019/12) and was carried out at the Chemistry Department of same University.

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