Synthesis of some NH-derivatives of ciprofloxacin as antibacterial and antifungal agents
DOI:
https://doi.org/10.3329/bjp.v6i1.7720Keywords:
Antibacterial, Antifungal, Ciprofloxacin, Schotten-Baumann methodAbstract
Five NH-derivatives of ciprofloxacin (2-6) have been prepared by acetylation/benzoylation on ciprofloxacin (1) in order to carry out screening for antibacterial activities on some Gram-positive and Gram-negative bacteria. The antifungal activity of these compounds has also been made against Candida albicans. All of the derivatives have shown enhanced activities against Gram-negatives bacteria than parent antibiotic, ciprofloxacin among which compounds 2 and 6 are the most potent agents. Regarding the antifungal activity all of the compounds have shown highest activity than ciprofloxacin. All the compounds have been characterized with spectral analysis.
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References
Bennish ML, Salam MA, Khan WA, Khan AM. Treatment of shigellosis: III. Comparison of one-or-two-dose ciprofloxacin with standard 5 day therapy: A randomized, blinded trial. Ann Intern Med. 1992; 117: 727-34.
Crumplin GC, Smith JT. Nalidixic acid bacterial chromosome replication. Nature 1976; 260: 643-45
de Souza NJ, Gupte SV, Deshpande PK, Desai VN, Bhawsar SB, Yeole RD, Shukla MC, Strahilevitz J, Hooper DC, Bozdogan B, Appelbaum PC, Jacobs MR, Shetty N, Patel MV, Jha R, Khorakiwala HF. A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus. J Med Chem. 2005; 48: 5232-42.
Devnath HP, Islam MR. Synthesis of some pyrazolone derivatives from ciprofloxacin and study of their cytotoxicity. Bangladesh J Pharmacol. 2010; 5: 30-33.
Goots TD, Brighty KE. Fluoroquinolone antibacterials: SAR, mechanism of action, resistance and clinical aspects. Med Res Rev. 1996; 16: 433-86.
Hooper DC, Wolfson JS. Fluoroquinolone antibacterial agents. N Engl J Med. 1991; 324: 384-94.
Jubie S, Sikdar P, Kalirajan R, Gowramma B, Gomaathy S, Sankar S, Elanga K. Synthesis and antimicrobial activity of some novel ciprofloxacin analogues. J Pharma Res. 2010; 3: 511-13.
Ludlam HA, Barton I, White L, McMullin C, King A, Phillips I. Intraperitoneal ciprofloxacin for the treatment of peritonitis in patients receiving continuous ambulatory peritoneal dialysis (CAPD). J Antimicrob Chemother. 1990; 25: 843-51.
Peterson LR, Lissack LM, Canter K, Fasching CE, Clabots C, Gerding. DN. Therapy of lower extremity infections with ciprofloxacin in patients with diabetes mellitus, peripheral vascular disease, or both. Am J Med. 1989; 86: 801-08.
Siddiqui R, Sultana N, Khan KM, Akbar N, Ali M, Arayne S. Effects of skeletal modifications of ciprofloxacin on antibacterial, antifungal and cytotoxic activities. J Chinese Clin Med. 2007; 21: 188-95.
Wang JC. DNA topoisomerases. Annu Rev Biochem. 1985; 54: 665-97.
Yamashita Y, Ashizawa T, Morimoto M, Hosomi J, Nakano H. Antitumor quinolones with mammalian topoisomerase II mediated DNA cleavage activity. Cancer Res. 1992; 52: 2818-22.
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