Leishmanicidal Activity of New Megazol Derivatives

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).

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