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  • Title: Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues.
    Author: Aher NG, Pore VS, Mishra NN, Kumar A, Shukla PK, Sharma A, Bhat MK.
    Journal: Bioorg Med Chem Lett; 2009 Feb 01; 19(3):759-63. PubMed ID: 19110424.
    Abstract:
    Fluconazole based novel mimics containing 1,2,3-triazole were designed and synthesized as antifungal agents. Their antifungal activities were evaluated in vitro by measuring the minimal inhibitory concentrations (MICs). Compounds 12, 15, and 16 were found to be more potent against Candida fungal pathogens than control drugs fluconazole and amphotericin B. The studies presented here provide structural modification of fluconazole to give 1,2,3-trazole containing molecules. Furthermore, these molecules were evaluated in vivo against Candida albicans intravenous challenge in Swiss mice and antiproliferative activities were tested against human hepatocellular carcinoma Hep3B and human epithelial carcinoma A431. It was found that compound 12 resulted in 97.4% reduction in fungal load in mice and did not show any profound proliferative effect at lower dose (0.001 mg/ml).
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