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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

New Limonene-Hybrid Derivatives with Anti-T. cruzi Activity

Author(s): G. Alvarez, A. Gerpe, D. Benitez, F. Garibotto, S. Zacchino, C. S. Graebin, R. Gomes da Rosa, V. L. Eifler-Lima, M. Gonzalez and H. Cerecetto

Volume 7, Issue 6, 2010

Page: [452 - 460] Pages: 9

DOI: 10.2174/157018010791306524

Price: $65

Abstract

The development of hybrid compounds containing limonene- and recognized anti-T. cruzi-heterocycleframeworks is described. The six new compounds displayed broad antitrypanosomal activities having 5-nitrofuran and 5- nitroindazole derivatives, the best profiles. In addition, a 5-nitroindazole derivative evaluated against a panel of fungi exhibited relevant activities. Knowing that free-radical-production operates as one of the mechanisms of action on these heterocycles, we studied a potential extra-mechanism, membrane-sterols changes. Non-relevant T. cruzi squalene accumulation was observed for any of the tested hybrid-limonene derivatives.

Keywords: Limonene derivatives, Anti-T. cruzi agents, Antifungal, Lipinski rule, 5-nitrofuran, 5-nitroindazole


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