title: Evaluation of α,β-unsaturated ketones as antileishmanial agents.
abstract: In this study, we assessed the antileishmanial activity of 126 α,β-unsaturated ketones. The compounds NC901, NC884, and NC2459 showed high leishmanicidal activity for both the extracellular (50% effective concentration [EC50], 456 nM, 1,122 nM, and 20 nM, respectively) and intracellular (EC50, 1,870 nM, 937 nM, and 625 nM, respectively) forms of Leishmania major propagated in macrophages, with little or no toxicity to mammalian cells. Bioluminescent imaging of parasite replication showed that all three compounds reduced the parasite burden in the murine model, with no apparent toxicity.
authors: Border Biomedical Research Center, Department of Biological Sciences, The University of Texas at El Paso, El Paso, Texas, USA.
authors: Miguel A
authors: MA
authors: Vasquez
authors: Border Biomedical Research Center, Department of Biological Sciences, The University of Texas at El Paso, El Paso, Texas, USA.
authors: Eva
authors: E
authors: Iniguez
authors: College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan, Canada.
authors: Umashankar
authors: U
authors: Das
authors: Department of Molecular Microbiology, Washington University School of Medicine, St. Louis, Missouri, USA.
authors: Stephen M
authors: SM
authors: Beverley
authors: Border Biomedical Research Center, Department of Biological Sciences, The University of Texas at El Paso, El Paso, Texas, USA.
authors: Linda J
authors: LJ
authors: Herrera
authors: College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan, Canada.
authors: Jonathan R
authors: JR
authors: Dimmock
authors: Border Biomedical Research Center, Department of Biological Sciences, The University of Texas at El Paso, El Paso, Texas, USA ramaldonado@utep.edu.
authors: Rosa A
authors: http://orcid.org/0000-0003-3180-7192
authors: RA
authors: Maldonado
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D007659:Ketones / Q000737:chemistry / Q000494:pharmacology*; D018320:Leishmania major / Q000187:drug effects*; D008264:Macrophages / Q000469:parasitology*; D051379:Mice
chemical_list: D000981:Antiprotozoal Agents; D007659:Ketones