4.6 Article

Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 7, Issue 20, Pages 4163-4165

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/b911483a

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Funding

  1. NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [P50GM067082] Funding Source: NIH RePORTER
  2. NIGMS NIH HHS [P50 GM067082-07, P50 GM067082] Funding Source: Medline

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Two novel SF(5) 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 SF(5)-substituted quinolines.

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