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Milner, E.; McCalmont, W.; Bhonsle, J.; Caridha, D.; Cobar, J.; Gardner, S.; Gerena, L.; Goodine, D.; Lanteri, C.; Melendez, V.; Roncal, N.; Sousa, J.; Wipf, P.; Dow, G. Anti-malarial activity of a non-piperidine library of next-generation quinoline methanols Malar. J. 2010, 9, 51
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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.; Tangteung, A.; Wipf, P.; Dow, G. Structure-activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparum Bioorg. Med. Chem. Lett. 2010, 20, 1347-1351
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Dow, G.; Milner, E.; Bathurst, I; Bhonsle, J.; Caridha, D.; Gardner, S.; Gerena, L.; Kozar, M.; Lanteri, C.; Mannila, A.; McCalmont, W.; Melendez, V.; Moon, J.; Read, K.; Norval, S.; Roncal, N.; Shackleford, D.; Sousa, J.; Stouten, J.; White, K.; Zeng, Q.; Charman, S. Central nervous system (CNS) exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous (IV) dosing in mice Malar. J. 2011, 10, 150
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Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine
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Wipf, P.; Mo, T.; Geib, S.; Caridha, D.; Dow, G.; Gerena, L.; Roncal, N.; Milner, E. Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine Org. Biomol. Chem. 2009, 7, 4163-4165
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Initially (+)- and (-)-enantiomers of epoxide 3 were obtained via supercritical fluid chromatographic separation performed by Regis Technology (; refer to Supporting Information for chromatogram). Once a lead candidate was declared, the bulk synthesis of the corresponding (+) enantiomer of epoxide 3 was out-sourced to Bioblocks (http://www.bioblocks.com).
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Initially (+)- and (-)-enantiomers of epoxide 3 were obtained via supercritical fluid chromatographic separation performed by Regis Technology (http://www.registech.com; refer to Supporting Information for chromatogram). Once a lead candidate was declared, the bulk synthesis of the corresponding (+) enantiomer of epoxide 3 was out-sourced to Bioblocks (http://www.bioblocks.com).
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Lee, P.11
Leed, S.12
Norval, S.13
Tungtaeng, A.14
Zeng, Q.15
Kozar, M.16
Read K, D.17
Li, Q.18
Dow, G.19
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United States Food and Drug Administration, Center for Drug Evaluation and Research. United States Department of Health and Human Services: Washington, DC.
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United States Food and Drug Administration, Center for Drug Evaluation and Research. Development of New Stereoisomeric Drugs; United States Department of Health and Human Services: Washington, DC, 2005; http://www.fda.gov/Drugs/ GuidanceComplianceRegulatoryInformation/Guidances/.
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Plasma concentrations of sulfadoxine-pyrimethamine and of mefloquine during regular long term malaria prophylaxis
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DOI 10.1016/0035-9203(90)90376-P
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Hellgren, U.; Angel, V. H.; Bergvist, Y; Arvidsson, A.; Forero-Gomez, J. S.; Rombo, L. Plasma concentrations of sulfadoxine-pyrimethamine and of mefloquine during regular long term malaria prophylaxis Trans. R. Soc. Trop. Med. Hyg. 1990, 84, 46-49 (Pubitemid 20062549)
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80052810896
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The tables in the article were developed using SAR Vision software, info@chemapps.com.
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The tables in the article were developed using SAR Vision software, info@chemapps.com.
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