Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice

Geoffrey Dow; Erin Milner; Ian Bathurst; Jayendra Bhonsle; Diana Caridha; Sean Gardner; Lucia Gerena; Michael Kozar; Charlotte Lanteri; Anne Mannila; William McCalmont; Jay Moon; Kevin Read; Suzanne Norval; Norma Roncal; David Shackleford; Jason Sousa; Jessica Steuten; Karen White; Qiang Zeng; Susan Charman

doi:10.1186/1475-2875-10-150

Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice

Geoffrey Dow, Erin Milner, Ian Bathurst, Jayendra Bhonsle, Diana Caridha, Sean Gardner, Lucia Gerena, Michael Kozar, Charlotte Lanteri, Anne Mannila, William McCalmont, Jay Moon, Kevin Read, Suzanne Norval, Norma Roncal, David Shackleford, Jason Sousa, Jessica Steuten, Karen White, Qiang ZengSusan Charman

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19 Citations (Scopus)

Abstract

The clinical use of mefloquine (MQ) has declined due to dose-related neurological events. Next generation quinoline methanols (NGQMs) that do not accumulate in the central nervous system (CNS) to the same extent may have utility. In this study, CNS levels of NGQMs relative to MQ were measured and an early lead chemotype was identified for further optimization.

Original language	English
Pages (from-to)	e1 - e11
Number of pages	11
Journal	Malaria Journal
Volume	10
Issue number	150
DOIs	https://doi.org/10.1186/1475-2875-10-150
Publication status	Published - 2011

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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., Moon, J., Read, K., Norval, S., Roncal, N., Shackleford, D., Sousa, J., Steuten, J., White, K., ... Charman, S. (2011). Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice. Malaria Journal, 10(150), e1 - e11. https://doi.org/10.1186/1475-2875-10-150

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title = "Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice",

abstract = "The clinical use of mefloquine (MQ) has declined due to dose-related neurological events. Next generation quinoline methanols (NGQMs) that do not accumulate in the central nervous system (CNS) to the same extent may have utility. In this study, CNS levels of NGQMs relative to MQ were measured and an early lead chemotype was identified for further optimization.",

author = "Geoffrey Dow and Erin Milner and Ian Bathurst and Jayendra Bhonsle and Diana Caridha and Sean Gardner and Lucia Gerena and Michael Kozar and Charlotte Lanteri and Anne Mannila and William McCalmont and Jay Moon and Kevin Read and Suzanne Norval and Norma Roncal and David Shackleford and Jason Sousa and Jessica Steuten and Karen White and Qiang Zeng and Susan Charman",

year = "2011",

doi = "10.1186/1475-2875-10-150",

language = "English",

volume = "10",

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journal = "Malaria Journal",

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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, Moon, J, Read, K, Norval, S, Roncal, N, Shackleford, D, Sousa, J, Steuten, J, White, K, Zeng, Q & Charman, S 2011, 'Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice', Malaria Journal, vol. 10, no. 150, pp. e1 - e11. https://doi.org/10.1186/1475-2875-10-150

TY - JOUR

T1 - Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice

AU - Dow, Geoffrey

AU - Milner, Erin

AU - Bathurst, Ian

AU - Bhonsle, Jayendra

AU - Caridha, Diana

AU - Gardner, Sean

AU - Gerena, Lucia

AU - Kozar, Michael

AU - Lanteri, Charlotte

AU - Mannila, Anne

AU - McCalmont, William

AU - Moon, Jay

AU - Read, Kevin

AU - Norval, Suzanne

AU - Roncal, Norma

AU - Shackleford, David

AU - Sousa, Jason

AU - Steuten, Jessica

AU - White, Karen

AU - Zeng, Qiang

AU - Charman, Susan

PY - 2011

Y1 - 2011

N2 - The clinical use of mefloquine (MQ) has declined due to dose-related neurological events. Next generation quinoline methanols (NGQMs) that do not accumulate in the central nervous system (CNS) to the same extent may have utility. In this study, CNS levels of NGQMs relative to MQ were measured and an early lead chemotype was identified for further optimization.

AB - The clinical use of mefloquine (MQ) has declined due to dose-related neurological events. Next generation quinoline methanols (NGQMs) that do not accumulate in the central nervous system (CNS) to the same extent may have utility. In this study, CNS levels of NGQMs relative to MQ were measured and an early lead chemotype was identified for further optimization.

UR - http://www.malariajournal.com/content/10/1/150

U2 - 10.1186/1475-2875-10-150

DO - 10.1186/1475-2875-10-150

M3 - Article

SN - 1475-2875

VL - 10

SP - e1 - e11

JO - Malaria Journal

JF - Malaria Journal

IS - 150

ER -

Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice

Abstract

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