Journal
LETTERS IN DRUG DESIGN & DISCOVERY
Volume 13, Issue 10, Pages 1063-1075Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1570180813666160819151239
Keywords
Synthesis; aminoguanidine; 1,3,4-oxadiazol; piperazine; 3-amine-1,2,4-triazole; antibacterial activity
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Funding
- National Science Foundation of China [81260468, 81360473, 81460524]
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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 antibacterial 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 mu g/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 mu g/mL. These two compounds also displayed significant antifungal activity against Candida albicans 7535 with MIC value of 1 mu g/mL, which were equivalent to MIC value of 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.
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