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Synthesis and antibacterial activity of N-1 substituted Fluoroquinolones.
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| Author:
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UPLOADED BY-ADMIN, AKHILES ROY, SHAILESH SHAH, DINESH SHAH, SANDESH LODHA, GAJANAN KALYANKAR
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| Abstract:
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Fluoroquinolones are the fastest growing antibacterial class in terms of global revenue.
Current development of fluoroquinolones is based on structure activity relationship while
pointing out to their mode of action. However, increased indiscriminate prescribing has led to
recent occasional emergence of fluoroquinolone resistant bacteria, which necessitated the
search for newer drugs with efficacy against resistant strains. Present work was taken up as a
part of worldwide effort to synthesize newer fluoroquinolones having better efficacy, lesser
side effects and well tolerability than the available ones. N-1 position is important for overall
potency of the molecule so the synthesized nucleus was substituted at N-1 position with newer
substituents. Microwave assisted synthesis of fluoroquinolone nucleus was adopted for better
yield, lesser time and purity reasons. The compounds were screened for antibacterial activity
by Bauer Kirby method (Disc Method) against E.coli, S.aureus, and P.aeruginosa.
Compounds showed moderate activity as compared to Ciprofloxacin.
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| Keyword:
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Fluoroquinolones, Resistance, Microwave, Antibacterial, Disc method
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| EOI:
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| DOI:
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