Synthesis and antifungal activity of 1,5-disubstituted-1,2,3-triazole containing fluconazole analogues

MedChemComm
2012.0

Abstract

Fluconazole based novel mimics containing 1,5-disubstituted 1,2,3-triazoles were synthesized by using Ru catalysed 1,3 dipolar cycloaddition. All the newly synthesized compounds and pure enantiomers were more potent than fluconazole against Candida albicans. Docking of 9A and 9B showed different conformation in the active site of Cyp51 of Candida albicans. The more active compounds 2 and 2A did not exhibit any toxicity up to 3.12 mg mL1 against mammalian cell line L929.

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