The results of experiments in dogs with and without two glucose loads and in the isolated pancreas to compare the pharmacodynamics of two low-dosage arylsulphonylureas, glipizide and glibenclamide, are described and discussed.-The results agree with those obtained by other authors confirming that glibenclamide shows delayed but prolonged activity on both plasma insulin and glucose levels. Moreover glibenclamide counteracts the hyperglycaemia induced by the second glucose load less effieently. Glipizide acts faster on insulin and glucose levels, which return quickly to normal. When a second glucose load was given it was still more active in reducing plasma glucose levels. The dynamics of insulin secretion following glipizide more closely resembles tolbutamide than glibenelamide.
Die Reaktion der Säurechloride, Ester oder Azide (I) mit p‐(β‐Aminoäthyl)‐ benzolsulfonamid (II) führt zu den Acylaminosulfonamiden (III), die mit Cyclohexylisocyanat (IV) zu den Sulfonylharnstoffen (V) weiter umgesetzt werden.
Die teils im Handel erhältlichen, teils nach bekannten Methoden dargestellten heterocyclischen Carbonsäuren (I) werden meist über die gemischten Anhydride (II) ‐ in einigen Fällen über die Säurechloride oder Azide ‐ durch Einwirkung von p‐(β‐Aminoäthyl)‐benzolsulfonamid (III) in die Carbonsäureamide (IV) und dann durch Reaktion mit Cyclohexylisocyanat (V) in die Sulfonylharnstoffe (VI) umgewandelt.
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