Rational Synthesis, Photophysical and Biochemical Evaluation of Fluorescents Chalcones as Inhibitors of Cruzain from Trypanosoma cruzi

Rational Synthesis, Photophysical and Biochemical Evaluation of Fluorescents Chalcones as Inhibitors of Cruzain from Trypanosoma cruzi

Silva, Wender A.; Melo, Lennine R.; Oliveira, Guilherme R.; Silva, Camilla C. C.; Trossini, Gustavo H. G.

Abstract:

Chagas’ disease is an infection caused by the protozoan parasite Trypanosoma cruzi, considered by World Health Organization as a neglected disease it causes thousands of deaths each year. Only drugs, nifurtimox and benznidazole, are using against this disease, however it are effective just in the acute phase and are highly toxic. Thus, new drugs are urgently needed. Cruzain, a cysteine protease, has been selected as an attractive target for the development of new antitrypanosomal agents. In this context, chalcones (1,3-diaryl-2- propen-1-ones) belong to the flavonoid family, and commonly possess interesting biological activities, as reviewed elsewhere, have presented a promising inhibitory activity against cruzain.

Chagas’ disease is an infection caused by the protozoan parasite Trypanosoma cruzi, considered by World Health Organization as a neglected disease it causes thousands of deaths each year. Only drugs, nifurtimox and benznidazole, are using against this disease, however it are effective just in the acute phase and are highly toxic. Thus, new drugs are urgently needed. Cruzain, a cysteine protease, has been selected as an attractive target for the development of new antitrypanosomal agents. In this context, chalcones (1,3-diaryl-2- propen-1-ones) belong to the flavonoid family, and commonly possess interesting biological activities, as reviewed elsewhere, have presented a promising inhibitory activity against cruzain.

Palavras-chave:

DOI: 10.5151/chempro-15bmos-BMOS2013_2013915192751

Referências bibliográficas

• [1] 1 Z. Nowakowska, Eur. J. Med. Chem., 2007, 42, 125.
• [2] 2Sajid, M.; McKerrow, J. H. Mol. Biochem Parasitol. 2002, 1221, 159.
• [3] 3.M.; Xavier, M. E.; Soares, T. A.; Gomes, A. F.; Gozzo, F. C.; Silva, W. A.;
• [4] Neto, B. A. D. Org. Biomol. Chem., 2013, 11, 4764.
• [5] 4Borchhardt, D. M.; Mascarello, A.; Chiaradia, L. D.; Nunes, R. J.; Oliva, G.;
• [6] Yunes, R. A.; Andricopulo, A. D. J. Braz. Chem. Soc. 2010, 21,142.

Como citar:

Silva, Wender A.; Melo, Lennine R.; Oliveira, Guilherme R.; Silva, Camilla C. C.; Trossini, Gustavo H. G.; "Rational Synthesis, Photophysical and Biochemical Evaluation of Fluorescents Chalcones as Inhibitors of Cruzain from Trypanosoma cruzi", p-265-265. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 2, Dezembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-15bmos-BMOS2013_2013915192751