Synthesis and biological evaluation of trifluralin analogues as antileishmanial agents

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 Leishma...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2010, Vol.18 (1), p.274-281
Main Authors: Esteves, M.A., Fragiadaki, I., Lopes, R., Scoulica, E., Cruz, M.E.M.
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Antiprotozoal Agents - chemical synthesis
Antiprotozoal Agents - chemistry
Antiprotozoal Agents - pharmacology
Biological activity
Biological and medical sciences
Cell Death - drug effects
Cell Line
Dinitroanilines
Erythrocytes - drug effects
Hemolysis - drug effects
Humans
Leishmania
Leishmania - drug effects
Leishmania donovani
Leishmania donovani - drug effects
Leishmania infantum
Leishmania infantum - drug effects
Leishmaniasis - drug therapy
Medical sciences
Pharmacology. Drug treatments
Trifluralin - chemical synthesis
Trifluralin - chemistry
Trifluralin - pharmacology
Trifluralin analogues
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Summary: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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2009.10.059