Literature DB >> 21450374

Synthesis and anti-Trypanosoma cruzi activity of β-lapachone analogues.

Sabrina Baptista Ferreira1, Kelly Salomão, Fernando de Carvalho da Silva, Antônio Ventura Pinto, Carlos Roland Kaiser, Angelo C Pinto, Vitor Francisco Ferreira, Solange L de Castro.   

Abstract

The available chemotherapy for Chagas disease, caused by Trypanosoma cruzi, is unsatisfactory; therefore, there is an intense effort to find new drugs for the treatment of this disease. In our laboratory, we have analyzed the effect on bloodstream trypomastigotes of 16 new naphthoquinone analogues of β-lapachone modified in the pyran ring, aiming to find a new prototype with high trypanocidal activity. The new compounds presented a broad spectrum of activity, and five of them presented IC(50)/24 h in the range of 22-63 μM, whereas β-lapachone had a higher value of 391.5 ± 16.5 μM.
Copyright © 2011 Elsevier Masson SAS. All rights reserved.

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Year:  2011        PMID: 21450374     DOI: 10.1016/j.ejmech.2011.03.012

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   7.088


  12 in total

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