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• W2766002858 abstract "We describe the discovery and optimization of new, brain-penetrant T-type calcium channel blockers. We present optimized compounds with excellent efficacy in a rodent model of generalized absence-like epilepsy. Along the fine optimization of a chemical series with a pharmacological target located in the CNS (target potency, brain penetration, and solubility), we successfully identified an Ames negative aminopyrazole as putative metabolite of this compound series. Our efforts culminated in the selection of compound 20, which was elected as a preclinical candidate." @default.
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• W2766002858 date "2017-10-25" @default.
• W2766002858 modified "2023-09-27" @default.
• W2766002858 title "Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies" @default.
• W2766002858 doi "https://doi.org/10.2533/chimia.2017.722" @default.
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