@article{ef05a8dded0d467bbc7a65c90f28ebc0,
title = "Quinolone-3-diarylethers: A new class of antimalarial drug",
abstract = "The goal for developing new antimalarial drugs is to find a molecule that can target multiple stages of the parasite's life cycle, thus impacting prevention, treatment, and transmission of the disease. The 4(1H)-quinolone-3- diarylethers are selective potent inhibitors of the parasite's mitochondrial cytochrome bc1 complex. These compounds are highly active against the human malaria parasites Plasmodium falciparum and Plasmodium vivax. They target both the liver and blood stages of the parasite as well as the forms that are crucial for disease transmission, that is, the gametocytes, the zygote, the ookinete, and the oocyst. Selected as a preclinical candidate, ELQ-300 has good oral bioavailability at efficacious doses in mice, is metabolically stable, and is highly active in blocking transmission in rodent models of malaria. Given its predicted low dose in patients and its predicted long half-life, ELQ-300 has potential as a new drug for the treatment, prevention, and, ultimately, eradication of human malaria.",
keywords = "4(1h) quinolone 3 diarylether derivative, amodiaquine, antimalarial agent, artesunate, atovaquone, chloroquine, elq 271, elq 300, gsk 932121a, mefloquine, p 4q 391, piperaquine, proguanil, ubiquinol cytochrome c reductase, unclassified drug, animal cell, animal experiment, animal model, antimalarial activity, apicomplexan life cycle stage, area under the curve, article, controlled study, drug bioavailability, drug clearance, drug cytotoxicity, drug distribution, drug efficacy, drug half life, drug mechanism, drug potency, drug potentiation, drug safety, drug selectivity, drug sensitivity, drug structure, enzyme inhibition, ex vivo study, female, gametocyte, human, human cell, IC 50, in vitro study, in vivo study, low drug dose, malaria, malaria control, malaria falciparum, mouse, nonhuman, parasite transmission, parasite vector, Plasmodium berghei, Plasmodium falciparum, Plasmodium vivax, Plasmodium yoelii, priority journal, single drug dose, Animals, Antimalarials, Atovaquone, Drug Resistance, Drug Synergism, Life Cycle Stages, Malaria, Malaria, Falciparum, Mice, Proguanil, Pyridones, Quinolones",
author = "Aaron Nilsen and LaCrue, {Alexis N.} and White, {Karen L.} and Forquer, {Isaac P.} and Cross, {R. Matthew} and Jutta Marfurt and Mather, {Michael W.} and Delves, {Michael J.} and Shackleford, {David M.} and Saenz, {Fabian E.} and Morrisey, {Joanne M.} and Jessica Steuten and Tina Mutka and Yuexin Li and Grennady Wirjanata and Eileen Ryan and Sandra Duffy and Kelly, {Jane Xu} and Sebayang, {Boni F.} and Anne-Marie Zeeman and Rintis Noviyanti and Sinden, {Robert E.} and Kocken, {Clemens H M} and Price, {Ric N.} and Avery, {Vicky M.} and I{\~n}igo Angulo-Barturen and Jim{\'e}nez-D{\'i}az, {Mar{\'i}a Bel{\'e}n} and Santiago Ferrer and Esperanza Herreros and Sanz, {Laura Mar{\'i}a} and Gamo–Benito, {Francisco Javier} and Ian bathurst and Burrows, {Jeremy N.} and Peter Siegl and Guy, {R. Kiplin} and Winter, {Rolf W.} and Vaidya, {Akhil B.} and Charman, {Susan A.} and Kyle, {Dennis E.} and Roman Manetsch and Riscoe, {Michael K.}",
year = "2013",
month = mar
day = "20",
doi = "10.1126/scitranslmed.3005029",
language = "English",
volume = "5",
pages = "1--13",
journal = "Science Translational Medicine",
issn = "1946-6234",
publisher = "American Association for the Advancement of Science",
number = "177",
}