《利尿藥和降血糖藥》ppt課件-文庫吧
2024-12-24 04:11 本頁面
【正文】 n the urea nitrogen。 methyl and ethyl pounds are not active. Usually, there is only one (normally substituent para) on the sulfonyl aromatic ring. SNHNHROOOR 39。Many simple substituents on the sulfonyl aromatic ring are active. The p(βarylcarboxamidoethyl) grouping seen in second generation pounds is consistent with high potency. It is thought that the spatial relationship between the amide nitrogen of the substituent and the sulfonamide nitrogen is important. Tolbutamide N[(Butylamino)carbonyl]4methylbenzene –sulfonamide Butyl group on the urea nitrogen。 Paramethylbenzene on the sulfonyl group. SNHNHOOO Properties Tolbutamide have sulfonylurea structure with weak acid, and this property may be used for assay. Instability: Tolbutamide is hydrolyzed to paratoluene sulfonamide by acids. Heating of its filtrate with sodium hydroxide solution produces nbutylamine odour. Metabolism Tolbutamide is metabolized in the liver to phydroxyl tolbutamide, retaining about 35% of the activity of the parent pound. it is converted very rapidly to the inactive tolbutamide 4carboxylic acid. Glibenclamide ONHSNHNHC lOOOO5ChloroN[2[4[[[(cyclohexylamino)carbonyl] amino]sulfonyl]phenyl]2methoxybenzamide Introduction of cyclohexane on the urea nitrogen。 Introduction of side chain on the sulfonyl aromatic ring. Properties It is not stable to moisture and is hydrolyzed to sulfamide derivate. Metabolism Glibenclamide affords trans439。hydroxyglyburide as the major product. The 339。hydroxy metabolite retains about 15% of the activity of the parent pound. Therapeutic Application In general, the effects of the first and secondgeneration sulfonylureas are similar. All produce reliable hypoglycemia in type 2 diabetics. These agents work best in patients whose type 2 diabetes is relatively mild. Synthetic Route Thirdgeneration sulfonylurea Glimepiride is a sulfonylurea with a quick onset of action and a long duration of action. It may bind to a different protein in the putative sulfonylurea receptor than earlier drugs, and may exert it
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