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Targeting the fatty acid biosynthesis enzyme, beta-ketoacyl-acyl carrier protein synthase III (PfKASIII), in the identification of novel antimalarial agents.
Lee PJ, Bhonsle JB, Gaona HW, Huddler DP, Heady TN, Kreishman-Deitrick M, Bhattacharjee A, McCalmont WF, Gerena L, Lopez-Sanchez M, Roncal NE, Hudson TH, Johnson JD, Prigge ST, Waters NC. Lee PJ, et al. J Med Chem. 2009 Feb 26;52(4):952-63. doi: 10.1021/jm8008103. J Med Chem. 2009. PMID: 19191586 Free PMC article.
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. 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
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. 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. 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
Salicylanilide inhibitors of Toxoplasma gondii.
Fomovska A, Wood RD, Mui E, Dubey JP, Ferreira LR, Hickman MR, Lee PJ, Leed SE, Auschwitz JM, Welsh WJ, Sommerville C, Woods S, Roberts C, McLeod R. Fomovska A, et al. Among authors: lee pj. J Med Chem. 2012 Oct 11;55(19):8375-91. doi: 10.1021/jm3007596. Epub 2012 Sep 26. J Med Chem. 2012. PMID: 22970937 Free PMC article.
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
622 results