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Conformational restriction of methionyl tRNA synthetase inhibitors leading to analogues with potent inhibition and excellent gram-positive antibacterial activity.
Jarvest, Richard L; Berge, John M; Brown, Pamela; Houge-Frydrych, Catherine S V; O'Hanlon, Peter J; McNair, David J; Pope, Andrew J; Rittenhouse, Stephen.
Afiliación
  • Jarvest RL; GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK. richard_l_jarvest@gsk.com
Bioorg Med Chem Lett ; 13(7): 1265-8, 2003 Apr 07.
Article en En | MEDLINE | ID: mdl-12657260
Conformationally restricted analogues of the central linker unit of bacterial methionyl tRNA synthetase (MRS) inhibitors have been prepared. The (1S,2R)-cyclopentylmethyl moiety was identified as the preferred cyclic linker, with significant diastereo- and enantioselectivity of activity. Combination of this linker with an optimal substituted aryl right-hand side has resulted in a compound with exceptionally good antibacterial activity against staphylococci and enterococci, including antibiotic resistant strains.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores Enzimáticos / Bacterias Grampositivas / Metionina-ARNt Ligasa / Antibacterianos Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2003 Tipo del documento: Article Pais de publicación: Reino Unido
Buscar en Google
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores Enzimáticos / Bacterias Grampositivas / Metionina-ARNt Ligasa / Antibacterianos Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2003 Tipo del documento: Article Pais de publicación: Reino Unido