Regioselective synthesis and antimicrobial studies of ester linked 1,4-disubstituted 1,2,3-bistriazoles

A series of 1,4-disubstituted 1,2,3-bistriazoles was synthesized via click chemistry and evaluated for antibacterial/antifungal activities. A series of 1,4-disubstituted 1,2,3-bistriazoles was synthesized via click chemistry by cycloaddition of various bisalkynes with benzyl/2-phenylethyl azide. Syn...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-07, Vol.22 (13), p.4353-4357
Main Authors: Lal, Kashmiri, Kumar, Ashwani, Pavan, M.S., Kaushik, C.P.
Format: Article
Language:English
Subjects:
1,4-Disubstituted 1,2,3-triazoles
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - chemistry
Anti-Infective Agents - pharmacology
Antibacterial activity
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal activity
Antifungal agents
antifungal properties
Bacteria - drug effects
Binding Sites
Biological and medical sciences
chemistry
Click Chemistry
Computer Simulation
Crystallography, X-Ray
DNA Gyrase - chemistry
DNA Gyrase - metabolism
DNA topoisomerase (ATP-hydrolysing)
Docking studies
Esters
Fungi - drug effects
Medical sciences
Molecular Conformation
nuclear magnetic resonance spectroscopy
Pharmacology. Drug treatments
Protein Structure, Tertiary
Stereoisomerism
triazoles
Triazoles - chemistry
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Summary:A series of 1,4-disubstituted 1,2,3-bistriazoles was synthesized via click chemistry and evaluated for antibacterial/antifungal activities. A series of 1,4-disubstituted 1,2,3-bistriazoles was synthesized via click chemistry by cycloaddition of various bisalkynes with benzyl/2-phenylethyl azide. Synthesized triazoles were characterized by IR, 1H NMR, 13C NMR and mass spectral techniques. All the compounds were evaluated for antibacterial/antifungal activities and found to possess moderate to good antimicrobial activities. Further the docking study for the most active compound against DNA Gyrase was also carried out.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.05.008