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

TitleSynthesis and antifungal activity of 1,5-disubstituted-1,2,3-triazole containing fluconazole analogues
Publication TypeJournal Article
Year of Publication2012
AuthorsPore, VS, Jagtap, MA, Agalave, SG, Pandey, AK, Siddiqi, MI, Kumar, V, Shukla, PK
JournalMedchemcomm
Volume3
Issue4
Pagination484-488
Date PublishedAPR
ISSN2040-2503
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 mu g mL(-1) against mammalian cell line L929.

DOI10.1039/c2md00205a
Type of Journal (Indian or Foreign)Foreign
Impact Factor (IF)2.722
Divison category: 
Organic Chemistry