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Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine.

ABSTRACT: Two novel SF5 analogs of the antimalarial agent mefloquine were synthesized in 5 steps and 10-23% overall yields and found to have improved activity and selectivity against malaria parasites. This work also represents the first report of SF5-substituted quinolines.

SUBMITTER: Wipf P

PROVIDER: S-EPMC2929370 | biostudies-literature | 2009 Oct

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine.

Wipf Peter P Mo Tingting T Geib Steven J SJ Caridha Diana D Dow Geoffrey S GS Gerena Lucia L Roncal Norma N Milner Erin E EE

Organic & biomolecular chemistry 20090807 20

Two novel SF5 analogs of the antimalarial agent mefloquine were synthesized in 5 steps and 10-23% overall yields and found to have improved activity and selectivity against malaria parasites. This work also represents the first report of SF5-substituted quinolines. ...[more]

PMID: 19795052

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