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Structure-activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparum.
Milner E, McCalmont W, Bhonsle J, Caridha D, Carroll D, Gardner S, Gerena L, Gettayacamin M, Lanteri C, Luong T, Melendez V, Moon J, Roncal N, Sousa J, Tungtaeng A, Wipf P, Dow G. Milner E, et al. Among authors: mccalmont w. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1347-51. doi: 10.1016/j.bmcl.2010.01.001. Epub 2010 Jan 7. Bioorg Med Chem Lett. 2010. PMID: 20097070
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: mccalmont w. 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. Among authors: mccalmont w. J Med Chem. 2011 Sep 22;54(18):6277-85. doi: 10.1021/jm200647u. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21854078
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. Among authors: mccalmont wf. J Med Chem. 2009 Feb 26;52(4):952-63. doi: 10.1021/jm8008103. J Med Chem. 2009. PMID: 19191586 Free PMC article.
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: mccalmont w. Malar J. 2011 Jun 6;10:150. doi: 10.1186/1475-2875-10-150. Malar J. 2011. PMID: 21645370 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. Among authors: mccalmont w. 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
11 results