Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.

Ma, Dawei; Jiang, Yongwen; Chen, Fangping; Gong, Li-kun; Ding, Ke; Xu, Yong; Wang, Renxiao; Ge, Aihua; Ren, Jin; Li, Jingya; Li, Jia; Ye, Qizhuang

Ma, Dawei; Jiang, Yongwen; Chen, Fangping; Gong, Li-kun; Ding, Ke; Xu, Yong; Wang, Renxiao; Ge, Aihua; Ren, Jin; Li, Jingya; Li, Jia; Ye, Qizhuang.

Afiliación

Ma D; State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China. madw@mail.sioc.ac.cn

J Med Chem ; 49(2): 456-8, 2006 Jan 26.

Article en En | MEDLINE | ID: mdl-16420030

RESUMEN

The synthesis and matrix metalloproteinase (MMP) inhibitory activity of a series of gamma-keto carboxylic acids are described. Among nine MMP isozymes tested, compound 1j displays selective inhibition of MMP-2, -9, and -12 with IC(50) values between 0.20 and 1.51 microuM, and in male golden Syrian hamsters, it shows protection against PPE-induced emphysema.

Asunto(s)

Cetoácidos/síntesis química; Inhibidores de la Metaloproteinasa de la Matriz; Enfisema Pulmonar/prevención & control; Animales; Cricetinae; Isoenzimas/antagonistas & inhibidores; Isoenzimas/química; Cetoácidos/química; Cetoácidos/farmacología; Masculino; Metaloproteinasas de la Matriz/química; Mesocricetus; Modelos Moleculares; Elastasa Pancreática; Enfisema Pulmonar/inducido químicamente; Enfisema Pulmonar/enzimología; Relación Estructura-Actividad; Porcinos

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Banco de datos: MEDLINE Asunto principal: Enfisema Pulmonar / Inhibidores de la Metaloproteinasa de la Matriz / Cetoácidos Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2006 Tipo del documento: Article País de afiliación: China

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