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 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.
Esteves
M A
MA
Department of Chemical Industry Technologies, INETI, Estrada do Paço do Lumiar, 1649-038 Lisboa, Portugal.
Fragiadaki
I
I
Lopes
R
R
Scoulica
E
E
Cruz
M E M
ME
D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D004912:Erythrocytes / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D007891:Leishmania / Q000187:drug effects*; D007893:Leishmania donovani / Q000187:drug effects; D018314:Leishmania infantum / Q000187:drug effects; D007896:Leishmaniasis / Q000188:drug therapy*; D014274:Trifluralin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000981:Antiprotozoal Agents; D014274:Trifluralin