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Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles† †The authors declare no competing interests. ‡ ‡Electronic supplementary information (ESI) available: Detailed experimental procedures. Copies of 1H and 13C NMR spectra of all new products. See DOI: 10.1039/c7md00008a

A series of prenyl 1,2,3-triazoles were prepared from isoprenyl azides and different alkynes. Most of the compounds were active against T. cruzi and L. donovani . A series of prenyl 1,2,3-triazoles were prepared from isoprenyl azides and different alkynes. The dipolar cycloaddition reaction provided...

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Published in:MedChemComm 2017-03, Vol.8 (5), p.1015-1021
Main Authors: Porta, Exequiel O. J., Jäger, Sebastián N., Nocito, Isabel, Lepesheva, Galina I., Serra, Esteban C., Tekwani, Babu L., Labadie, Guillermo R.
Format: Article
Language:English
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Summary:A series of prenyl 1,2,3-triazoles were prepared from isoprenyl azides and different alkynes. Most of the compounds were active against T. cruzi and L. donovani . A series of prenyl 1,2,3-triazoles were prepared from isoprenyl azides and different alkynes. The dipolar cycloaddition reaction provided exclusively primary azide products as regioisomeric mixtures that were separated by column chromatography and then fully characterized. Most of the compounds displayed antiparasitic activity against Trypanosoma cruzi and Leishmania donovani . The most active compounds were assayed as potential Tc CYP51 inhibitors.
ISSN:2040-2503
2040-2511
DOI:10.1039/c7md00008a