Synthesis and Antimicrobial Evaluation of Aminoguanidine and 3-amino- 1,2,4-triazole Derivatives as Potential Antibacterial Agents

Author(s): Tian-Yi Zhang, Chao Li, Ya-Ru Li, Xiao-Zhen Li, Liang-Peng Sun, Chang-Ji Zheng, Hu-Ri Piao

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 10 , 2016

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Graphical Abstract:


A series of aminoguanidine derivatives bearing a 1,3,4-oxadiazole or piperazine moiety has been synthesized and fully characterized together with a series of 3-amino-1,2,4-triazole derivatives, and the resulting compounds were evaluated for their anti-bacterial activity. Most of these compounds showed broad-spectrum antibacterial activities against both Gram-positive and Gram-negative bacteria with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values in the range of 1–64 μg/mL, including multidrug-resistant clinical isolates and a fungus. Notably, compounds 19e and 19f exhibited higher levels of activity than gatifloxacin and moxifloxacin against several methicillin-resistant Staphylococcus aureus (3167 and 3506) and quinolone-resistant S. aureus (3505 and 3519) strains with MIC and MBC values in the range of 1–2 µg/mL. These two compounds also displayed significant antifungal activities with MIC values of 1 μg/mL against Candida albicans 7535, which were equivalent to the MIC value of the standard drug fluconazole. These results therefore indicate that aminoguanidine derivatives that do not contain a piperazine moiety are interesting scaffolds for the development of novel antibacterial agents.

Keywords: Synthesis, aminoguanidine, 1, 3, 4-oxadiazol, piperazine, 3-amine-1, 2, 4-triazole, antibacterial activity.

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Article Details

Year: 2016
Published on: 30 October, 2016
Page: [1063 - 1075]
Pages: 13
DOI: 10.2174/1570180813666160819151239
Price: $65

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