Literature DB >> 17445951

Synthesis and evaluation of new difluoromethyl azoles as antileishmanial agents.

Sabrina B Ferreira1, Marilia S Costa, Núbia Boechat, Rômulo J S Bezerra, Marcelo S Genestra, Marilene M Canto-Cavalheiro, Warner B Kover, Vitor F Ferreira.   

Abstract

Several compounds of great pharmacological interest contain the triazole and imidazole rings. In order to find new drugs with antileishmanial activity we have synthesized and evaluated new imidazole and triazole compounds carrying either the carbaldehyde or the difluoromethylene functionalities against promastigote forms of Leishmania amazonensis. Among the compounds tested difluoromethylene azoles 4b and 8f have inhibited the parasite growth significantly. Our results show that the introduction of the difluoromethylene moieties has turned the inactive carbaldehydes into active antileishmanial compounds.

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Year:  2007        PMID: 17445951     DOI: 10.1016/j.ejmech.2007.02.020

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  9 in total

1.  Tandem synthesis of 1-formyl-1,2,3-triazoles.

Authors:  James T Fletcher; Joseph A Christensen; Eric M Villa
Journal:  Tetrahedron Lett       Date:  2017-10-13       Impact factor: 2.415

Review 2.  Computational studies on the regioselectivity of metal-catalyzed synthesis of 1,2,3 triazoles via click reaction: a review.

Authors:  Tayebeh Hosseinnejad; Bahareh Fattahi; Majid M Heravi
Journal:  J Mol Model       Date:  2015-09-18       Impact factor: 1.810

3.  2-Chloro-6,6-dimethyl-5,6-dihydro-indazolo[2,3-c]quinazoline.

Authors:  Núbia Boechat; Adriana Dos Santos Lages; Warner B Kover; Edward R T Tiekink; James L Wardell; Solange M S V Wardell
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-02-06

4.  N-(4-Chloro-phen-yl)ethanimidamide.

Authors:  Nubia Boechat; Warner B Kover; Sabrina B Ferreira; Solange M S V Wardell; James L Wardell; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-03-27

5.  Novel synthesis of pseudopeptides bearing a difluoromethyl group by Ugi reaction and desulfanylation.

Authors:  Jingjing Wu; Hui Li; Song Cao
Journal:  Beilstein J Org Chem       Date:  2011-08-08       Impact factor: 2.883

6.  [1-(3-Chloro-phen-yl)-1H-1,2,3-triazol-4-yl]methanol hemihydrate.

Authors:  Nübia Boechat; Maria de Lourdes G Ferreira; Monica M Bastos; James L Wardell; Solange M S V Wardell; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-10-12

7.  In vitro screening of known drugs identified by scaffold hopping techniques shows promising leishmanicidal activity for suramin and netilmicin.

Authors:  Supriya Khanra; Y Pavan Kumar; Jyotirmayee Dash; Rahul Banerjee
Journal:  BMC Res Notes       Date:  2018-05-21

Review 8.  The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines.

Authors:  Luiz C S Pinheiro; Lívia M Feitosa; Marilia O Gandi; Flávia F Silveira; Nubia Boechat
Journal:  Molecules       Date:  2019-11-13       Impact factor: 4.411

9.  Antivenom effects of 1,2,3-triazoles against Bothrops jararaca and Lachesis muta snakes.

Authors:  Thaisa F S Domingos; Laura de A Moura; Carla Carvalho; Vinícius R Campos; Alessandro K Jordão; Anna C Cunha; Vitor F Ferreira; Maria Cecília B V de Souza; Eladio F Sanchez; André L Fuly
Journal:  Biomed Res Int       Date:  2013-04-22       Impact factor: 3.411

  9 in total

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