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

Wipf, Peter; Mo, Tingting; Geib, Steven J; Caridha, Diana; Dow, Geoffrey S; Gerena, Lucia; Roncal, Norma; Milner, Erin E

Wipf, Peter; Mo, Tingting; Geib, Steven J; Caridha, Diana; Dow, Geoffrey S; Gerena, Lucia; Roncal, Norma; Milner, Erin E.

Afiliación

Wipf P; Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA. pwipf@pitt.edu

Org Biomol Chem ; 7(20): 4163-5, 2009 Oct 21.

Article en En | MEDLINE | ID: mdl-19795052

ABSTRACT

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.

Asunto(s)

Antimaláricos/síntesis química; Antimaláricos/farmacología; Mefloquina/síntesis química; Mefloquina/farmacología; Animales; Antimaláricos/química; Antimaláricos/toxicidad; Mefloquina/análogos & derivados; Mefloquina/toxicidad; Modelos Moleculares; Conformación Molecular; Plasmodium falciparum/efectos de los fármacos

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Mefloquina / Antimaláricos Límite: Animals Idioma: En Revista: Org Biomol Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: Estados Unidos

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