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N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.
Musso, D L; Andersen, M W; Andrews, R C; Austin, R; Beaudet, E J; Becherer, J D; Bubacz, D G; Bickett, D M; Chan, J H; Conway, J G; Cowan, D J; Gaul, M D; Glennon, K C; Hedeen, K M; Lambert, M H; Leesnitzer, M A; McDougald, D L; Mitchell, J L; Moss, M L; Rabinowitz, M H; Rizzolio, M C; Schaller, L T; Stanford, J B; Tippin, T; Warner, J R; Whitesell, L G; Wiethe, R W.
Afiliación
  • Musso DL; GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709, USA. dm12907@glaxowellcome.com
Bioorg Med Chem Lett ; 11(16): 2147-51, 2001 Aug 20.
Article en En | MEDLINE | ID: mdl-11514157
ABSTRACT
N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which have potent broad-spectrum activity versus matrix metalloproteases and TNF-alpha converting enzyme (TACE). Compound 13c possesses good oral and intravenous pharmacokinetics in the rat and dog.
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Banco de datos: MEDLINE Asunto principal: Oligopéptidos / Metaloendopeptidasas / Inhibidores Enzimáticos / Inhibidores de la Metaloproteinasa de la Matriz / Formamidas Límite: Animals Idioma: En Año: 2001 Tipo del documento: Article
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Banco de datos: MEDLINE Asunto principal: Oligopéptidos / Metaloendopeptidasas / Inhibidores Enzimáticos / Inhibidores de la Metaloproteinasa de la Matriz / Formamidas Límite: Animals Idioma: En Año: 2001 Tipo del documento: Article