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Characterization of in vivo metabolites of WR319691, a novel compound with activity against Plasmodium falciparum.
Milner E, Sousa J, Pybus B, Melendez V, Gardner S, Grauer K, Moon J, Carroll D, Auschwitz J, Gettayacamin M, Lee P, Leed S, McCalmont W, Norval S, Tungtaeng A, Zeng Q, Kozar M, Read KD, Li Q, Dow G. Milner E, et al. Among authors: kozar m. Eur J Drug Metab Pharmacokinet. 2011 Sep;36(3):151-8. doi: 10.1007/s13318-011-0047-8. Epub 2011 Jul 13. Eur J Drug Metab Pharmacokinet. 2011. PMID: 21751074
Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice.
Dow GS, Milner E, Bathurst I, Bhonsle J, Caridha D, Gardner S, Gerena L, Kozar M, Lanteri C, Mannila A, McCalmont W, Moon J, Read KD, Norval S, Roncal N, Shackleford DM, Sousa J, Steuten J, White KL, Zeng Q, Charman SA. Dow GS, et al. Among authors: kozar m. Malar J. 2011 Jun 6;10:150. doi: 10.1186/1475-2875-10-150. Malar J. 2011. PMID: 21645370 Free PMC article.
Structure-activity relationships of 4-position diamine quinoline methanols as intermittent preventative treatment (IPT) against Plasmodium falciparum.
Milner E, Gardner S, Moon J, Grauer K, Auschwitz J, Bathurst I, Caridha D, Gerena L, Gettayacamin M, Johnson J, Kozar M, Lee P, Leed S, Li Q, McCalmont W, Melendez V, Roncal N, Sciotti R, Smith B, Sousa J, Tungtaeng A, Wipf P, Dow G. Milner E, et al. Among authors: kozar m. J Med Chem. 2011 Sep 22;54(18):6277-85. doi: 10.1021/jm200647u. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21854078
Ketotifen is an antimalarial prodrug of norketotifen with blood schizonticidal and liver-stage efficacy.
Milner E, Sousa J, Pybus B, Auschwitz J, Caridha D, Gardner S, Grauer K, Harris E, Hickman M, Kozar MP, Lee P, Leed S, Li Q, Melendez V, Moon J, Ngundam F, O'Neil M, Parriott S, Potter B, Sciotti R, Tangteung A, Dow GS. Milner E, et al. Among authors: kozar mp. Eur J Drug Metab Pharmacokinet. 2012 Mar;37(1):17-22. doi: 10.1007/s13318-012-0080-2. Eur J Drug Metab Pharmacokinet. 2012. PMID: 22314893
The use of a prodrug approach to minimize potential CNS exposure of next generation quinoline methanols while maintaining efficacy in in vivo animal models.
Sousa JC, Milner E, Carroll D, McCalmont W, Gardner S, Moon J, Johnson JD, Lee P, Auschwitz J, Roncal N, Caridha D, Tungteung A, Zeng Q, Reyes S, Smith B, Li Q, Kozar MP, Melendez V, Dow G. Sousa JC, et al. Eur J Drug Metab Pharmacokinet. 2014 Dec;39(4):231-6. doi: 10.1007/s13318-013-0162-9. Epub 2014 Apr 7. Eur J Drug Metab Pharmacokinet. 2014. PMID: 24705994
New imidazolidinedione derivatives as antimalarial agents.
Zhang L, Sathunuru R, Luong T, Melendez V, Kozar MP, Lin AJ. Zhang L, et al. Bioorg Med Chem. 2011 Feb 15;19(4):1541-9. doi: 10.1016/j.bmc.2010.12.028. Epub 2010 Dec 16. Bioorg Med Chem. 2011. PMID: 21282058
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