1. Search for factors affecting antibacterial activity and toxicity of 1,2,4-triazole-ciprofloxacin hybrids.
- Author
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Plech T, Kaproń B, Paneth A, Kosikowska U, Malm A, Strzelczyk A, Stączek P, Świątek Ł, Rajtar B, and Polz-Dacewicz M
- Subjects
- Anti-Bacterial Agents chemistry, Anti-Bacterial Agents pharmacology, Ciprofloxacin chemistry, Ciprofloxacin pharmacology, Gram-Negative Bacteria drug effects, Gram-Positive Bacteria drug effects, HEK293 Cells, Humans, Inhibitory Concentration 50, Microbial Sensitivity Tests, Molecular Structure, Structure-Activity Relationship, Triazoles chemistry, Triazoles pharmacology, Anti-Bacterial Agents chemical synthesis, Ciprofloxacin chemical synthesis, Triazoles chemical synthesis
- Abstract
A series of 1,2,4-triazole-based compounds was designed as potential antibacterial agents using molecular hybridization approach. The target compounds (23-44) were synthesized by Mannich reaction of 1,2,4-triazole-3-thione derivatives with ciprofloxacin (CPX) and formaldehyde. Their potent antibacterial effect on Gram-positive bacteria was accompanied by similarly strong activity against Gram-negative strains. The toxicity of the CPX-triazole hybrids for bacterial cells was even up to 18930 times higher than the toxicity for human cells. The results of enzymatic studies showed that the antibacterial activity of the CPX-triazole hybrids is not dependent solely on the degree of their affinity to DNA gyrase and topoisomerase IV., (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)
- Published
- 2015
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