Synthesis and biological evaluation of trifluralin analogues as antileishmanial agents

Bioorganic & Medicinal Chemistry
M A EstevesM E Cruz

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.

References

Nov 10, 2004·Drug Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy·Marc OuelletteBarbara Papadopoulou

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Citations

Jul 10, 2012·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Rui M LopesM Eugénia M Cruz
Oct 11, 2011·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·R LopesA J Almeida
Sep 12, 2015·European Journal of Medicinal Chemistry·Rémi CaraballoMikael Elofsson
Jul 15, 2015·Nanomedicine : Nanotechnology, Biology, and Medicine·Maria Manuela GasparMaria Eugénia Meirinhos Cruz
Jul 30, 2014·Phytotherapy Research : PTR·Fetene AbejeKaleab Asres
May 6, 2015·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Manuela CarvalheiroM Eugénia M Cruz
Feb 18, 2014·International Journal for Parasitology. Drugs and Drug Resistance·Marta G SilvaCarlos E Suarez
Jan 6, 2011·Expert Opinion on Therapeutic Patents·Biswa Prasun ChatterjiDulal Panda
Apr 14, 2020·Drug Design, Development and Therapy·Markos TadeleAsrat Hailu
Feb 4, 2021·Drug Delivery and Translational Research·Manuela CarvalheiroSandra Simões
Sep 26, 2014·Chemical Reviews·Hidayat HussainSimon Gibbons

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