| Autor: |
Silva RS; Núcleo de Pesquisas em Produtos Naturais, CCS, Universidade Federal do Rio de Janeiro, Brazil., Costa EM, Trindade UL, Teixeira DV, Pinto Mde C, Santos GL, Malta VR, De Simone CA, Pinto AV, de Castro SL |
| Jazyk: |
angličtina |
| Zdroj: |
European journal of medicinal chemistry [Eur J Med Chem] 2006 Apr; Vol. 41 (4), pp. 526-30. Date of Electronic Publication: 2006 Feb 28. |
| DOI: |
10.1016/j.ejmech.2005.12.006 |
| Abstrakt: |
Four new naphthofuranquinones, obtained from 2-hydroxy-3-allyl-naphthoquinone (1) and nor-lapachol (2), have their structures established by physical and X-ray analysis and their activity evaluated against Trypanosoma cruzi. Compounds 3 and 4 were obtained by addition of iodine to 1 followed by cyclization generating a furan ring. Compound 5 was obtained through the acid-catalyzed reaction by dissolution of 1 in sulfuric acid. Compound 6 was synthesized by addition of bromine and aniline to 2. The IC(50)/24 h for 3-6 in assays with T. cruzi trypomastigotes was between 157 and 640 microM, while the value for crystal violet was 536.0 +/- 3.0 microM. Compounds 3-5 also inhibited epimastigote proliferation. The trypanocidal activity of the new naphthofuranquinones endowed with redox properties reinforces a rational approach in the chemotherapy of Chagas' disease. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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