| Literature DB >> 20378360 |
Eufrânio N da Silva1, Tiago T Guimarães, Rubem F S Menna-Barreto, Maria do Carmo F R Pinto, Carlos A de Simone, Claudia Pessoa, Bruno C Cavalcanti, José R Sabino, Carlos Kleber Z Andrade, Marilia O F Goulart, Solange L de Castro, Antônio V Pinto.
Abstract
In continuing our screening program of naphthoquinone activity against Trypanosoma cruzi, the aetiological agent of Chagas' disease, new beta-lapachone-based 1,2,3-triazoles, 3-arylamino-nor-beta-lapachones, 3-alkoxy-nor-beta-lapachones and imidazole anthraquinones were synthesised and evaluated against bloodstream trypomastigote forms of the parasite. Compounds 2,2-dimethyl-3-(2,4-dibromophenylamino)-2,3-dihydro-naphtho[1,2-b]furan-4,5-dione, IC(50)/24h 24.9+/-7.4 and 4-azido-3-bromo-2,2-dimethyl-3,4-dihydro-2H-benzo[h]chromene-5,6-dione with 23.4+/-3.8 microM showed a trypanosomicidal activity higher than benznidazole. These results demonstrate the potential of naphthoquinone derivatives as novel structures for the development of alternative drugs for Chagas' disease. (c) 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20378360 DOI： 10.1016/j.bmc.2010.03.029
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.461