1,1-diósidos de 1,2,5-tiadiazol y 1,2,6-tiadiazina: Síntesis ractividad y aplicaciones a la obtención de nuevos agentes antihistamínicos H2.

Abstract

El descubrimiento de la burimamida por Black y colaboradores¹ en 1972 constituye el primer paso del desarrollo de los antagonistas de los receptores H₂ de histamina. Este compuesto, aunque de baja actividad, condujo por variación estructural a otros antagonistas más potentes. De hecho, la metiamida², y sobre todo la cimetidina³,4, la ranitidina y la famotidina se han usado en los úl- timos años en el tratamiento de trastornos gástricos asociados a la hiperclorhidria. La eficacia clíni- ca de estos compuestos ha supuesto un gran estímulo, que ha impulsado la obtención de otros fár- macos de este tipo dotados de mayor actividad y duración de acción y con menores efectos secun- darios.

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The discovery of burimamide by Black et al.¹ in 1972 constitutes the first step in the development of histamine H₂ receptor antagonists. This compound, although of low activity, led by structural variation to other more potent antagonists. In fact, methyamide², and especially cimetidine³,4, ranitidine and famotidine have been used in recent years in the treatment of gastric disorders associated with hyperchlorhydria. The clinical efficacy of these compounds has been a great stimulus, which has prompted the obtaining of other drugs of this type with greater activity and duration of action and with fewer side effects.