Design, synthesis and biological evaluation of ciprofloxacin tethered bis-1,2,3-triazole conjugates as potent antibacterial agents

Eur J Med Chem. 2016 Nov 29:124:218-228. doi: 10.1016/j.ejmech.2016.08.031. Epub 2016 Aug 17.

Abstract

A series of new bis-1,2,3-triazole linked ciprofloxacin conjugates was designed, synthesized and evaluated in vitro antibacterial activity against a panel of clinically relevant bacteria. A significant part of the compounds displayed enhanced activity against both Gram-positive and Gram-negative species of bacteria as compared to the parent drug. Additionally, negligible toxicity profile of compounds indicates that they may act a good antibiotic in future. Despite relatively small number of synthesized conjugates, it was possible to observe important dependences between their structure and activity.

Keywords: 1,2,3-Triazole conjugates; Antibacterial activity; Ciprofloxacin; Hemotoxicity.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / toxicity
  • Chemistry Techniques, Synthetic
  • Ciprofloxacin / chemical synthesis*
  • Ciprofloxacin / chemistry
  • Ciprofloxacin / pharmacology*
  • Ciprofloxacin / toxicity
  • Drug Design*
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Hemolysis / drug effects
  • Humans
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship
  • Triazoles / chemistry*

Substances

  • Anti-Bacterial Agents
  • Triazoles
  • Ciprofloxacin