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Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles.


ABSTRACT: 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 fully characterized. Most of the compounds displayed antiparasitic activity against Trypanosoma cruzi and Leishmania donovani. The most active compounds were assayed as potential TcCYP51 inhibitors.

SUBMITTER: Porta EOJ 

PROVIDER: S-EPMC5629980 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature

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Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles.

Porta Exequiel O J EOJ   Jäger Sebastián N SN   Nocito Isabel I   Lepesheva Galina I GI   Serra Esteban C EC   Tekwani Babu L BL   Labadie Guillermo R GR  

MedChemComm 20170310 5


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 fully characterized. Most of the compounds displayed antiparasitic activity against <i>Trypanosoma cruzi</i> and <i>Leishmania donovani</i>. The most active compounds were assayed as potential <i>Tc</i>CYP51 inhibitors. ...[more]

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