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Issue 23, 2015
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Design and synthesis of new fluconazole analogues

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Abstract

We have synthesized new fluconazole analogues containing two different 1,2,3-triazole units in the side chain. The synthesis of new amide analogues using a variety of acids is also described. All the compounds showed very good antifungal activity. A hemolysis study of the most active compounds 6e and 13j showed that both compounds did not cause any hemolysis at the dilutions tested. These compounds did not exhibit any toxicity to L929 cells at MIC and lower concentrations. In the docking study, the overall binding mode of 6e and 13j appeared to be reasonable and provided a good insight into the structural basis of inhibition of Candida albicans Cyp51 by these compounds.

Graphical abstract: Design and synthesis of new fluconazole analogues

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Publication details

The article was received on 25 Mar 2015, accepted on 30 Apr 2015 and first published on 01 May 2015


Article type: Paper
DOI: 10.1039/C5OB00590F
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Org. Biomol. Chem., 2015,13, 6551-6561

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    Design and synthesis of new fluconazole analogues

    V. S. Pore, S. G. Agalave, P. Singh, P. K. Shukla, V. Kumar and M. I. Siddiqi, Org. Biomol. Chem., 2015, 13, 6551
    DOI: 10.1039/C5OB00590F

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