DOI QR코드

DOI QR Code

Synthesis, Characterization and Biological Evaluations of Ciprofloxacin Carboxamide Analogues

  • Sultana, Najma (Department of Pharmaceutical Chemistry, Research Institute of Pharmaceutical Sciences, Faculty of Pharmacy, University of Karachi) ;
  • Arayne, Muhammad Saeed (Department of Chemistry, University of Karachi) ;
  • Rizvi, Syeda Bushra Shakeb (Department of Pharmaceutical Chemistry, Faculty of Pharmacy Federal Urdu University of Arts, Science and Technology) ;
  • Haroon, Urooj (Department of Chemistry, Federal Urdu University of Arts, Science and Technology)
  • 투고 : 2010.06.23
  • 심사 : 2010.11.30
  • 발행 : 2011.02.20

초록

Present work comprises of synthesis various analogues of ciprofloxacin by introducing new functionality at carboxylic group position via ester aminolysis reaction. For this purpose the carboxylic group at C-3 was esterified and later subjected to nucleophilic attack at the carbonyl carbon by various aromatic amines. Structure of the analogues was confirmed by different techniques i.e. IR, $^1H$ NMR and mass spectrometry. The antibacterial activity of the derivatives was also assessed with the parent against a series of Gram-positive and Gram-negative bacteria. The synthesized compounds showed diverse antimicrobial profile among which most compounds possessed a comparable or better activity in comparison to the ciprofloxacin. Additionally unlike ciprofloxacin, some of the derivatives were also found to show antifungal activity.

키워드

참고문헌

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피인용 문헌

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  3. 4-Quinolone Derivatives and Their Activities Against Gram-negative Pathogens vol.55, pp.9, 2018, https://doi.org/10.1002/jhet.3244
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  5. Total Syntheses of Lobaric Acid and Its Derivatives from the Antarctic Lichen Stereocaulon alpinum vol.81, pp.6, 2018, https://doi.org/10.1021/acs.jnatprod.8b00227
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  7. Theoretical molecular predictions and antimicrobial activities of newly synthesized molecular hybrids of norfloxacin and ciprofloxacin vol.57, pp.1, 2011, https://doi.org/10.1002/jhet.3768