Bioorganic & Medicinal Chemistry 2010-01-01

Synthesis and biological evaluation of trifluralin analogues as antileishmanial agents.

M A Esteves, I Fragiadaki, R Lopes, E Scoulica, M E M Cruz

Index: Bioorg. Med. Chem. 18 , 274-81, (2010)

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Abstract

A series of new analogues of trifluralin (TFL) were synthesized and characterized in view of changing the unfavorable properties that limits its use as antileishmanial agent. Some of the TFL analogues display more activity than a standard drug (miltefosine) against the promastigote forms of Leishmania infantum and Leishmania donovani and the intracellular form (THP-1 infected with L. infantum). All analogues showed a clear advantage over miltefosine, as they are not hemolytic. Some analogues can conjugate these characteristics with reduced cell toxicity and improved intracellular activity.Copyright (c) 2009 Elsevier Ltd. All rights reserved.