Leishmanicidal Activity of New Megazol Derivatives

Author(s): R. R. Riente, V. P. Souza, S. A. Carvalho, M. Kaiser, R. Brun, E. F. da Silva.

Journal Name: Medicinal Chemistry

Volume 5 , Issue 4 , 2009

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Abstract:

A series of thirteen new megazol derivatives, designed exploring the molecular hybridization approach between megazol (3) and heterocombretastatins (2), was synthesized. These new compounds were tested for in vitro antiparasitic activity upon axenic amastigotes of Leishmania donovani. Biological results led us to identify a new potent megazol derivative (4g), which presents an IC50 = 0.081μg/mL, more active tham the reference drug miltefosine (IC50 = 0.131μg/mL).

Keywords: Leishmanicidal, megazol derivatives, molecular hybridization, heterocombretastatin, cytotoxic, sulfones

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Article Details

VOLUME: 5
ISSUE: 4
Year: 2009
Page: [392 - 397]
Pages: 6
DOI: 10.2174/157340609788681467
Price: $58

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