Literature DB >> 15095419

Novel antiprotozoal products: imidazole and benzimidazole N-oxide derivatives and related compounds.

Gabriela Aguirre1, Mariana Boiani, Hugo Cerecetto, Alejandra Gerpe, Mercedes González, Yolanda Fernández Sainz, Ana Denicola, Carmen Ochoa De Ocáriz, Juan José Nogal, David Montero, José Antonio Escario.   

Abstract

The syntheses and biological evaluation of the first anti-protozoa imidazole N-oxide and benzimidazole N-oxide and their derivatives are reported. They were tested in vitro against two different protozoa, Trypanosoma cruzi and Trichomonas vaginalis. Derivative 7c, ethyl-1-(i-butyloxycarbonyloxy)-6-nitrobenzimid-azole-2-carboxylate, displayed activity on both protozoa. Lipophilicity and redox potential were experimentally determined in order to study the relationship with activity of the compounds. These properties are well related with the observed bioactivity. Imidazole and benzimidazole N-oxide derivatives are becoming leaders for further chemical modifications and advanced biological studies.

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Year:  2004        PMID： 15095419     DOI： 10.1002/ardp.200300840

Source DB:  PubMed          Journal:  Arch Pharm (Weinheim)        ISSN： 0365-6233            Impact factor:   3.751


  8 in total

1.  Inhibitory potential of a novel imidazole derivative as evaluated by time-kill and dehydrogenase activity.

Authors:  Florin Aonofriesei; Simona Lupsor
Journal:  Curr Microbiol       Date:  2012-10-25       Impact factor: 2.188

2.  In vitro and in vivo activities of 1,3,4-thiadiazole-2-arylhydrazone derivatives of megazol against Trypanosoma cruzi.

Authors:  K Salomão; E M de Souza; S A Carvalho; E F da Silva; C A M Fraga; H S Barbosa; S L de Castro
Journal:  Antimicrob Agents Chemother       Date:  2010-03-15       Impact factor: 5.191

3.  Application of linear discriminant analysis in the virtual screening of antichagasic drugs through trypanothione reductase inhibition.

Authors:  Julián J Prieto; Alan Talevi; Luis E Bruno-Blanch
Journal:  Mol Divers       Date:  2006-09-21       Impact factor: 2.943

4.  A dynamic and electrostatic potential prediction of the prototropic tautomerism between imidazole 3-oxide and 1-hydroxyimidazole in external electric field.

Authors:  Yong Wang; Fu-de Ren; Duan-Lin Cao
Journal:  J Mol Model       Date:  2019-10-28       Impact factor: 1.810

5.  Screening of Potential anti-Trypanosoma cruzi Candidates: In Vitro and In Vivo Studies.

Authors:  Maria de Nazaré C Soeiro; Solange Lisboa de Castro
Journal:  Open Med Chem J       Date:  2011-03-09

6.  One-Pot Two-Step Synthesis of 2-Aryl benzimidazole N-oxides Using Microwave Heating as a Tool.

Authors:  Fabrizio Politano; Ana K Gran-Magano; Nicholas E Leadbeater
Journal:  Molecules       Date:  2019-10-09       Impact factor: 4.411

Review 7.  Synthetic approaches and pharmaceutical applications of chloro-containing molecules for drug discovery: A critical review.

Authors:  Wan-Yin Fang; L Ravindar; K P Rakesh; H M Manukumar; C S Shantharam; Njud S Alharbi; Hua-Li Qin
Journal:  Eur J Med Chem       Date:  2019-04-10       Impact factor: 6.514

8.  Imidazole as a Promising Medicinal Scaffold: Current Status and Future Direction.

Authors:  Sahar S Alghamdi; Rasha S Suliman; Khlood Almutairi; Khawla Kahtani; Dimah Aljatli
Journal:  Drug Des Devel Ther       Date:  2021-07-29       Impact factor: 4.162
  8 in total

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