Synthesis and antibacterial activity of 4'',11-di-O-arylalkylcarbamoyl azithromycin derivatives.

Ma, Shutao; Jiao, Bo; Liu, Zhaopeng; Wang, Hui; Xian, Ruiqing; Zheng, Manjie; Lou, Hongxiang

Ma, Shutao; Jiao, Bo; Liu, Zhaopeng; Wang, Hui; Xian, Ruiqing; Zheng, Manjie; Lou, Hongxiang.

Afiliación

Ma S; Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, PR China.

Bioorg Med Chem Lett ; 19(6): 1698-701, 2009 Mar 15.

Article en En | MEDLINE | ID: mdl-19232491

ABSTRACT

ABSTRACT

A series of new 4'',11-di-O-arylalkylcarbamoyl azithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. Some derivatives exhibited greatly improved activity against erythromycin-resistant bacteria. Among them, compounds 5f and 5k were found to have potent activity against erythromycin-resistant Streptococcus pneumoniae whose resistance was encoded by the erm or mef gene.

Asunto(s)

Antibacterianos/síntesis química; Azitromicina/análogos & derivados; Química Farmacéutica/métodos; Antibacterianos/farmacología; Azitromicina/síntesis química; Azitromicina/farmacología; Proteínas Bacterianas/genética; Diseño de Fármacos; Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos; Farmacorresistencia Bacteriana Múltiple/genética; Macrólidos/química; Proteínas de la Membrana/genética; Metiltransferasas/genética; Pruebas de Sensibilidad Microbiana; Modelos Químicos; Infecciones Estreptocócicas/genética; Infecciones Estreptocócicas/prevención & control; Streptococcus pneumoniae/metabolismo

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Química Farmacéutica / Azitromicina / Antibacterianos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article

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