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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: melendez v. 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
New imidazolidinedione derivatives as antimalarial agents.
Zhang L, Sathunuru R, Luong T, Melendez V, Kozar MP, Lin AJ. Zhang L, et al. Among authors: melendez v. 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
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: melendez v. 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: melendez v. J Med Chem. 2011 Sep 22;54(18):6277-85. doi: 10.1021/jm200647u. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21854078
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
Dodean RA, Kancharla P, Li Y, Melendez V, Read L, Bane CE, Vesely B, Kreishman-Deitrick M, Black C, Li Q, Sciotti RJ, Olmeda R, Luong TL, Gaona H, Potter B, Sousa J, Marcsisin S, Caridha D, Xie L, Vuong C, Zeng Q, Zhang J, Zhang P, Lin H, Butler K, Roncal N, Gaynor-Ohnstad L, Leed SE, Nolan C, Huezo SJ, Rasmussen SA, Stephens MT, Tan JC, Cooper RA, Smilkstein MJ, Pou S, Winter RW, Riscoe MK, Kelly JX. Dodean RA, et al. Among authors: melendez v. J Med Chem. 2019 Apr 11;62(7):3475-3502. doi: 10.1021/acs.jmedchem.8b01961. Epub 2019 Mar 21. J Med Chem. 2019. PMID: 30852885 Free PMC article.
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: melendez v. 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. Among authors: melendez v. 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
Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.
Kancharla P, Dodean RA, Li Y, Pou S, Pybus B, Melendez V, Read L, Bane CE, Vesely B, Kreishman-Deitrick M, Black C, Li Q, Sciotti RJ, Olmeda R, Luong TL, Gaona H, Potter B, Sousa J, Marcsisin S, Caridha D, Xie L, Vuong C, Zeng Q, Zhang J, Zhang P, Lin H, Butler K, Roncal N, Gaynor-Ohnstad L, Leed SE, Nolan C, Ceja FG, Rasmussen SA, Tumwebaze PK, Rosenthal PJ, Mu J, Bayles BR, Cooper RA, Reynolds KA, Smilkstein MJ, Riscoe MK, Kelly JX. Kancharla P, et al. Among authors: melendez v. J Med Chem. 2020 Jun 11;63(11):6179-6202. doi: 10.1021/acs.jmedchem.0c00539. Epub 2020 May 26. J Med Chem. 2020. PMID: 32390431 Free PMC article.
47 results