Literature DB >> 28993794

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

Exequiel O J Porta1, Sebastián N Jäger1, Isabel Nocito2, Galina I Lepesheva3, Esteban C Serra2, Babu L Tekwani4, Guillermo R Labadie1,5.   

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.

Entities:  

Year:  2017        PMID： 28993794      PMCID： PMC5629980          DOI： 10.1039/C7MD00008A

Source DB:  PubMed          Journal:  Medchemcomm        ISSN： 2040-2503            Impact factor:   3.597


  26 in total

Review 1.  Screening strategies to identify new chemical diversity for drug development to treat kinetoplastid infections.

Authors:  Rob Don; Jean-Robert Ioset
Journal:  Parasitology       Date:  2013-08-28       Impact factor: 3.234

2.  Click chemistry decoration of amino sterols as promising strategy to developed new leishmanicidal drugs.

Authors:  Exequiel O J Porta; Paulo B Carvalho; Mitchell A Avery; Babu L Tekwani; Guillermo R Labadie
Journal:  Steroids       Date:  2013-11-04       Impact factor: 2.668

Review 3.  Macrocycles as potential therapeutic agents in neglected diseases.

Authors:  Stella Peña; Laura Scarone; Gloria Serra
Journal:  Future Med Chem       Date:  2015-02-04       Impact factor: 3.808

4.  Click-based synthesis and proteomic profiling of lipstatin analogues.

Authors:  Mun H Ngai; Peng-Yu Yang; Kai Liu; Yuan Shen; Markus R Wenk; Shao Q Yao; Martin J Lear
Journal:  Chem Commun (Camb)       Date:  2010-06-24       Impact factor: 6.222

Review 5.  Recent developments in rationally designed multitarget antiprotozoan agents.

Authors:  P M Njogu; K Chibale
Journal:  Curr Med Chem       Date:  2013       Impact factor: 4.530

6.  Complexes of Trypanosoma cruzi sterol 14α-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.

Authors:  Tatiana Y Hargrove; Zdzislaw Wawrzak; Paul W Alexander; Jason H Chaplin; Martine Keenan; Susan A Charman; Catherine J Perez; Michael R Waterman; Eric Chatelain; Galina I Lepesheva
Journal:  J Biol Chem       Date:  2013-09-18       Impact factor: 5.157

7.  Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth.

Authors:  Galina I Lepesheva; Robert D Ott; Tatiana Y Hargrove; Yuliya Y Kleshchenko; Inge Schuster; W David Nes; George C Hill; Fernando Villalta; Michael R Waterman
Journal:  Chem Biol       Date:  2007-11

8.  Synthesis of Farnesol Analogues Containing Triazoles in Place of Isoprenes through 'Click Chemistry'

Authors:  Thangaiah Subramanian; Sean Parkin; H Peter Spielmann
Journal:  Synlett       Date:  2012-10       Impact factor: 2.454

9.  Farnesyl diphosphate analogues with omega-bioorthogonal azide and alkyne functional groups for protein farnesyl transferase-catalyzed ligation reactions.

Authors:  Guillermo R Labadie; Rajesh Viswanathan; C Dale Poulter
Journal:  J Org Chem       Date:  2007-11-03       Impact factor: 4.354

10.  Chagas disease and the london declaration on neglected tropical diseases.

Authors:  Rick L Tarleton; Ricardo E Gürtler; Julio A Urbina; Janine Ramsey; Rodolfo Viotti
Journal:  PLoS Negl Trop Dis       Date:  2014-10-09
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  3 in total

1.  Repositioning Salirasib as a new antimalarial agent.

Authors:  Exequiel O J Porta; Ignasi Bofill Verdaguer; Consuelo Perez; Claudia Banchio; Mauro Ferreira de Azevedo; Alejandro M Katzin; Guillermo R Labadie
Journal:  Medchemcomm       Date:  2019-06-21       Impact factor: 3.597

2.  Synthesis, in vitro Antileishmanial Efficacy and Hit/Lead Identification of Nitrofurantoin-Triazole Hybrids.

Authors:  Nonkululeko H Zuma; Janine Aucamp; Maryna Viljoen; David D N'Da
Journal:  ChemMedChem       Date:  2022-05-02       Impact factor: 3.540

3.  Targeting L-Proline Uptake as New Strategy for Anti-chagas Drug Development.

Authors:  Lucía Fargnoli; Esteban A Panozzo-Zénere; Lucas Pagura; María Julia Barisón; Julia A Cricco; Ariel M Silber; Guillermo R Labadie
Journal:  Front Chem       Date:  2020-08-25       Impact factor: 5.221
  3 in total

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