Drug-induced modifications of the immune response. 12. 4,5-Dihydro-4-oxo-2-(substituted amino)-3-furancarboxylic acids and derivatives as novel antiallergic agents.

Mack, R A; Zazulak, W I; Radov, L A; Baer, J E; Stewart, J D; Elzer, P H; Kinsolving, C R; Georgiev, V S

Mack, R A; Zazulak, W I; Radov, L A; Baer, J E; Stewart, J D; Elzer, P H; Kinsolving, C R; Georgiev, V S.

Afiliación

Mack RA; Department of Organic Chemistry, Pennwalt Corporation, Rochester, New York 14623.

J Med Chem ; 31(10): 1910-8, 1988 Oct.

Article en En | MEDLINE | ID: mdl-3172125

RESUMEN

The synthesis of a series of novel 4,5-dihydro-4-oxo-2-(substituted amino)-3-furancarboxylic acids, salts, esters, and amides is described. The title compounds when tested in the mediator-induced dermal vascular permeability and active anaphylaxis assays in rats demonstrated moderate to potent antiallergic activity. The [2-trans-(4-methylphenyl)cyclopropyl]amino analogue 53 emerged as the most active derivative. Thus, when administered intraperitoneally to rats at a dose of 100 mg/kg, it inhibited the action of the mediators serotonin, histamine, and bradykinin by 100%. In the active anaphylaxis assay in rats, compound 30 suppressed the edema by 81% at a dose of 100 mg/kg, following intraperitoneal administration.

Asunto(s)

Formación de Anticuerpos/efectos de los fármacos; Hipersensibilidad/tratamiento farmacológico; Animales; Bradiquinina/farmacología; Permeabilidad Capilar/efectos de los fármacos; Furanos/farmacología; Histamina/farmacología; Ratas; Serotonina/farmacología; Relación Estructura-Actividad

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Hipersensibilidad / Formación de Anticuerpos Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 1988 Tipo del documento: Article Pais de publicación: Estados Unidos

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