Inhibitors of glycolic acid oxidase. 4-Substituted 3-hydroxy-1H-pyrrole-2, 5-dione derivatives

…, EJ Cragoe Jr, H Schwam, SR Michelson…

Index: Rooney; Randall; Streeter; Ziegler; Cragoe Jr.; Schwam; Michelson; Williams; Eichler; Duggan; Ulm; Noll Journal of Medicinal Chemistry, 1983 , vol. 26, # 5 p. 700 - 714

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Citation Number: 44

Abstract

An extensive series of novel 4-substituted 3-hydroxy-lH-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 lH- ...

~57%

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~45%

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~44%

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~93%

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