Tertiary amine pyrazolones and their salts as inhibitors of mutant superoxide dismutase 1-dependent protein aggregation for the treatment of amyotrophic lateral …

…, RJ Ferrante, RI Morimoto, RB Silverman

文献索引：Zhang, Yinan; Benmohamed, Radhia; Zhang, Wei; Kim, Jinho; Edgerly, Christina K.; Zhu, Yaoqiu; Morimoto, Richard I.; Ferrante, Robert J.; Kirsch, Donald R.; Silverman, Richard B. ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 7 p. 584 - 587

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被引用次数: 1

摘要

Pyrazolone derivatives have previously been found to be inhibitors of Cu/Zn superoxide dismutase 1 (SOD1)-dependent protein aggregation, which extended survival of an amyotrophic lateral sclerosis (ALS) mouse model. On the basis of ADME analysis, we describe herein a new series of tertiary amine-containing pyrazolones and their structure– activity relationships. Further conversion to the conjugate salts greatly improved their ...