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Repromicin derivatives with potent antibacterial activity against Pasteurella multocida.
McFarland, J W; Hecker, S J; Jaynes, B H; Jefson, M R; Lundy, K M; Vu, C B; Glazer, E A; Froshauer, S A; Hayashi, S F; Kamicker, B J; Reese, C P; Olson, J A.
Afiliación
  • McFarland JW; Central Research Division, Pfizer Inc., Groton, Connecticut 06340, USA. mcfarland@pfizer.com
J Med Chem ; 40(6): 1041-5, 1997 Mar 14.
Article en En | MEDLINE | ID: mdl-9083494
Reductive amination of repromicin with polyfunctional amines has led to new macrolide antibacterial agents, some of which are highly potent against the Gram-negative pathogen Pasteurella multocida both in vitro and in a mouse infection model. A key element in this discovery was the recognition that among certain known macrolides increasing lipophilicity results in diminished in vivo activity. One repromicin derivative, 20-[N-[3-(dimethylamino)-propyl]-N-L-alanylamino]-20-deoxorepro micin (35), was selected for advanced evaluation. At 5 mg/kg, a single subcutaneous dose was found to control induced pasteurellosis in swine and induced respiratory disease in cattle.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pasteurella multocida / Macrólidos / Antibacterianos Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 1997 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
Buscar en Google
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PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pasteurella multocida / Macrólidos / Antibacterianos Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 1997 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos