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The evaluation of quinonoid compounds against Trypanosoma cruzi: synthesis of imidazolic anthraquinones, nor-beta-lapachone derivatives and beta-lapachone-based 1,2,3-triazoles.

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.
AuthorsEufrânio N da Silva Jr, 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
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 18 Issue 9 Pg. 3224-30 (May 01 2010) ISSN: 1464-3391 [Electronic] England
PMID20378360 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Copyright(c) 2010 Elsevier Ltd. All rights reserved.
Chemical References
  • Anthraquinones
  • Antiparasitic Agents
  • Imidazoles
  • Naphthoquinones
  • Quinones
  • Triazoles
  • beta-lapachone
Topics
  • Animals
  • Anthraquinones (chemical synthesis, chemistry, pharmacology)
  • Antiparasitic Agents (chemical synthesis, chemistry, pharmacology)
  • Crystallography, X-Ray
  • Imidazoles (chemical synthesis, chemistry, pharmacology)
  • Mice
  • Molecular Structure
  • Naphthoquinones (chemical synthesis, chemistry, pharmacology)
  • Parasitic Sensitivity Tests
  • Quinones (chemical synthesis, chemistry, pharmacology)
  • Triazoles (chemical synthesis, chemistry, pharmacology)
  • Trypanosoma cruzi (drug effects)

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