Synthesis and antibacterial property of quinolines with potent DNA gyrase activity

Synthesis of a series of novel tetrahydroquinoline annulated heterocycles has been accomplished by intramolecular imino and bisimino Diels–Alder reaction. These compounds were evaluated for their antibacterial activity. All the synthetic compounds, exhibited good antibacterial activity against micro...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2009-01, Vol.17 (2), p.660-666
Main Authors: Ramesh, Ekambaram, Manian, Rathna Durga R.S., Raghunathan, Ragavachary, Sainath, Shilpakala, Raghunathan, Malathi
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Antibacterial
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Bisquinolone
Ciprofloxacin
Escherichia coli
Escherichia coli - drug effects
Gyrase
Medical sciences
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Quinolines - chemical synthesis
Quinolines - pharmacology
Quinolone
Structure-Activity Relationship
Topoisomerase II Inhibitors
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Summary:Synthesis of a series of novel tetrahydroquinoline annulated heterocycles has been accomplished by intramolecular imino and bisimino Diels–Alder reaction. These compounds were evaluated for their antibacterial activity. All the synthetic compounds, exhibited good antibacterial activity against microorganisms of which one of them 7 was found to be as active as the antibiotic ciplofloxacin and is found to have MIC value of 2.5 mg/mL against Escherichia coli.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2008.11.058