Design, synthesis and biological evaluation of ciprofloxacin tethered bis-1,2,3-triazole conjugates as potent antibacterial agents.
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.
Department of Medicinal Chemistry, Institute of Medical Sciences, Banaras Hindu University, Varanasi 221005, UP, India.
Rama
R
Kant
Department of Medicinal Chemistry, Institute of Medical Sciences, Banaras Hindu University, Varanasi 221005, UP, India.
Vishal
V
Singh
Department of Microbiology, Institute of Medical Sciences, Banaras Hindu University, Varanasi 221005, UP, India.
Gopal
G
Nath
Chemical Biology Research Laboratory, Department of Chemistry, University of Delhi, Delhi 110007, India.
Satish Kumar
SK
Awasthi
Department of Medicinal Chemistry, Institute of Medical Sciences, Banaras Hindu University, Varanasi 221005, UP, India. Electronic address: agarwal.dralka@gmail.com.
Alka
A
Agarwal
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D060326:Chemistry Techniques, Synthetic; D002939:Ciprofloxacin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D015195:Drug Design; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D014230:Triazoles; D002939:Ciprofloxacin
1,2,3-Triazole conjugates; Antibacterial activity; Ciprofloxacin; Hemotoxicity