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• W2401433182 abstract "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 solubility. Phosphate compound 17 exhibited numerous benefits both to cellular activity and to CNS-related drug-like properties in vitro and in vivo, including microsomal stability, tolerated toxicity, and blood-brain barrier permeation. These results indicate that tertiary amine pyrazolones comprise a valuable class of ALS drug candidates." @default.
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• W2401433182 date "2015-07-31" @default.
• W2401433182 modified "2023-10-13" @default.
• W2401433182 title "Tertiary Amine Pyrazolones and Their Salts as Inhibitors of Mutant Superoxide Dismutase 1-Dependent Protein Aggregation for the Treatment of Amyotrophic Lateral Sclerosis" @default.
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• W2401433182 doi "https://doi.org/10.1021/acs.jmedchem.5b00561" @default.
• W2401433182 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4537347" @default.
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