TY - JOUR
T1 - Evaluation of α,β-unsaturated ketones as antileishmanial agents
AU - Vasquez, Miguel A.
AU - Iniguez, Eva
AU - Das, Umashankar
AU - Beverley, Stephen M.
AU - Herrera, Linda J.
AU - Dimmock, Jonathan R.
AU - Maldonado, Rosa A.
N1 - Publisher Copyright:
Copyright © 2015, American Society for Microbiology. All Rights Reserved.
PY - 2015/6/1
Y1 - 2015/6/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=84929603687&partnerID=8YFLogxK
U2 - 10.1128/AAC.04056-14
DO - 10.1128/AAC.04056-14
M3 - Article
C2 - 25801571
AN - SCOPUS:84929603687
SN - 0066-4804
VL - 59
SP - 3598
EP - 3601
JO - Antimicrobial agents and chemotherapy
JF - Antimicrobial agents and chemotherapy
IS - 6
ER -