Die 7.011 J. T h i e l e und W. M a u c h o t ' ) beschriebeiie Di-neotriazoZcarbons~'ure liat sich als ein sehr geeignetes Ausgangsmaterial f~r das Studiam der Triazolverbindungen erwiesen. Voii ilir ausgchend, liabcn mir die folgende Untersuchung ausgefulirt. Was zunaclist die Constitution der DiaPotriuzolcarboIzsuzire, C,I-I,N,03, selbst betrifft, so ist sic seiner Zeit als iuneres Anhgdrid N-coo aufgefasst worden. Uiese Forniulirung lasst sich uicht niehr aufrecht erhalteii , denii a i r habeu jetzt gefundeii, dass auch der E'ster der Amidotriazolcarbonsaure eiiie analoge feste Dia z o~ erbindung licfert, bei wclcher von eincr solchen Anliydrid-' ) Diese Aniialeii 303, 33. Annnlen dei Chelnie 343. Bd.
An extensive series of novel 4-substituted 3-hydroxy-1H-pyrrole-2,5-dione derivatives has been prepared and studied as inhibitors of glycolic acid oxidase (GAO). Compounds possessing large lipophilic 4-substituents are, in general, potent, competitive inhibitors of porcine liver GAO in vitro. Methylation of the nitrogen or the 3-hydroxy substituent reduced potency dramatically, indicating the requirement for the two acidic functions on the 1H-pyrrole-2,5-dione nucleus. In rat liver perfusion studies, with three representative compounds, concentration-dependent inhibition of the conversion of [1-14C]glycolate to [14C]oxalate was observed. Chronic oral administration to ethylene glycol fed rats of the 4-(4'-bromo[1,1'-biphenyl]-4-yl) derivative (83) was shown to effect a significant reduction in urinary oxalate levels over a 58-day period.
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