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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15 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 languageEnglish
Pages (from-to)e1 - e11
Number of pages11
JournalMalaria Journal
Volume10
Issue number150
DOIs
Publication statusPublished - 2011

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