Issue 4, 2012
From the journal:

MedChemComm

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

Vandana S. Pore,*a   Manisha A. Jagtap,a   Sandip G. Agalave,a   Atindra K. Pandey,b   Mohammad I. Siddiqi,c   Vikash Kumarc  and  Praveen K. Shukla*b  

* Corresponding authors

a Organic Chemistry Division, National Chemical Laboratory, Pune, India
E-mail: vs.pore@ncl.res.in
Fax: +91-20-25902629
Tel: +91-20-25902320

b Medical Mycology Lab., Division of Fermentation Technology, CSIR, Central Drug Research Institute, Lucknow, India

c Computational Bio & Bioinformatics Lab., Molecular &Structural Biology Division, CSIR, Central Drug Research Institute, Lucknow, India

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 μg mL−1 against mammalian cell line L929.

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

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Article information

DOI
https://doi.org/10.1039/C2MD00205A
Article type
Concise Article
Submitted
09 Aug 2011
Accepted
20 Dec 2011
First published
25 Jan 2012

Med. Chem. Commun., 2012,3, 484-488

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

V. S. Pore, M. A. Jagtap, S. G. Agalave, A. K. Pandey, M. I. Siddiqi, V. Kumar and P. K. Shukla, Med. Chem. Commun., 2012, 3, 484 DOI: 10.1039/C2MD00205A

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