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Inotropic "A" ring substituted sulmazole and isomazole analogues.
Barraclough, P; Black, J W; Cambridge, D; Collard, D; Firmin, D; Gerskowitch, V P; Glen, R C; Giles, H; Hill, A P; Hull, R A.
Afiliación
  • Barraclough P; Department of Medicinal Chemistry, Wellcome Research Laboratories, Beckenham, Kent, U.K.
J Med Chem ; 33(8): 2231-9, 1990 Aug.
Article en En | MEDLINE | ID: mdl-2165165
A series of "A" ring substituted sulmazole and isomazole analogues have been prepared and evaluated as inotropic agents. pKA's, protonation sites, and log P values were measured for selected compounds and their electronic properties were calculated. No simple correlation between inotropic activity and pKA, protonation site, or log P value was observed. However, in vitro inotropism did correlate with the calculated charge density of the "B" ring imidazo nitrogen atom. The 6-position of sulmazole appeared to be the most tolerant toward substituents, the 6-amino derivative 7 being a more potent inotrope than sulmazole itself. 4-Methoxyisomazole 13 had comparable in vivo inotropic properties to those of isomazole.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Cardiotónicos / Imidazoles / Contracción Miocárdica Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 1990 Tipo del documento: Article Pais de publicación: Estados Unidos
Buscar en Google
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Imprimir
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PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Cardiotónicos / Imidazoles / Contracción Miocárdica Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 1990 Tipo del documento: Article Pais de publicación: Estados Unidos