Naphthoquinoidal [1,2,3]-triazole, a new structural moiety active against Trypanosoma cruzi
| Autor: | Antonio V. Pinto, Raphael S. F. Silva, Solange L. de Castro, Vitor F. Ferreira, Maria do Carmo F. R. Pinto, Eufranio N. Jr. da Silva, Daniel V. Teixeira, Carlos Alberto De Simone, Maria Cecília B. V. de Souza, Rubem F. S. Menna-Barreto |
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| Rok vydání: | 2007 |
| Předmět: |
Chagas disease
Models Molecular Azides 1 2 3-Triazole Stereochemistry Trypanosoma cruzi Triazole Crystallography X-Ray Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship Cations Drug Discovery medicine Moiety Structure–activity relationship Animals Pharmacology biology Molecular Structure Chemistry Organic Chemistry Hydrogen Bonding General Medicine Triazoles biology.organism_classification medicine.disease Trypanocidal Agents Quinone Naphthoquinones |
| Zdroj: | European journal of medicinal chemistry. 43(8) |
| ISSN: | 0223-5234 |
| Popis: | [1,2,3]-Triazole derivatives of nor-beta-lapachone were synthesized and assayed against the infective bloodstream trypomastigote form of Trypanosoma cruzi, the etiological agent of Chagas disease. All the derivatives were more active than the original quinones, with IC(50)/1 day values in the range of 17 to 359 microM, the apolar phenyl substituted triazole 6 being the most active compound. These triazole derivatives of nor-beta-lapachone emerge as interesting new lead compounds in drug development for Chagas disease. |
| Databáze: | OpenAIRE |
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