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
Medicinal Chemistry
Title: Leishmanicidal Activity of New Megazol Derivatives
Volume: 5 Issue: 4
Author(s): R. R. Riente, V. P. Souza, S. A. Carvalho, M. Kaiser, R. Brun and E. F. da Silva
Affiliation:
Keywords: Leishmanicidal, megazol derivatives, molecular hybridization, heterocombretastatin, cytotoxic, sulfones
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).
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Cite this article as:
Riente R. R., Souza P. V., Carvalho A. S., Kaiser M., Brun R. and da Silva F. E., Leishmanicidal Activity of New Megazol Derivatives, Medicinal Chemistry 2009; 5 (4) . https://dx.doi.org/10.2174/157340609788681467
DOI https://dx.doi.org/10.2174/157340609788681467 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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