High selective leishmanicidal activity of 3-hydroxy-2-methylene-3-(4-bromophenyl)propanenitrile and analogous compounds.

de Souza, R O M A; Pereira, V L P; Muzitano, M F; Falcão, C A B; Rossi-Bergmann, B; Filho, E B A; Vasconcellos, M L A A

de Souza, R O M A; Pereira, V L P; Muzitano, M F; Falcão, C A B; Rossi-Bergmann, B; Filho, E B A; Vasconcellos, M L A A.

Afiliación

de Souza RO; Núcleo de Pesquisas de Produtos Naturais, Universidade Federal do Rio de Janeiro, Bloco H, CCS, Ilha do Fundão, Rio de Janeiro, RJ 21941-590, Brazil.

Eur J Med Chem ; 42(1): 99-102, 2007 Jan.

Article en En | MEDLINE | ID: mdl-17010481

RESUMEN

Sixteen not new aromatic compounds were prepared by one-pot reaction i.e. through Baylis-Hillman reaction and were the first time evaluated against promastigote Leishmania amazonensis and infected mammalian cells. Most of the compounds were selectively more active against amastigotes than the reference drug sodium stibogluconate (Pentostam, IC(50)=44.7 microM). We found that 3-hydroxy-2-methylene-3-(4-bromophenyl) propanenitrile (13) was the most active (IC(50)=12.5 microM) and safer compound (0.0 (0.9); % macrophage LDH release), being the lead compound.

Asunto(s)

Leishmania/efectos de los fármacos; Nitrilos/síntesis química; Tripanocidas/síntesis química; Animales; Técnicas In Vitro; Macrófagos Peritoneales/efectos de los fármacos; Macrófagos Peritoneales/parasitología; Ratones; Nitrilos/química; Nitrilos/farmacología; Relación Estructura-Actividad; Tripanocidas/química; Tripanocidas/farmacología

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tripanocidas / Leishmania / Nitrilos Límite: Animals Idioma: En Revista: Eur J Med Chem Año: 2007 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Francia

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