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Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies
- Source :
- CHIMIA, Vol 71, Iss 10 (2017)
- Publication Year :
- 2017
- Publisher :
- Swiss Chemical Society, 2017.
-
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.
Details
- Language :
- German, English, French
- ISSN :
- 00094293 and 26732424
- Volume :
- 71
- Issue :
- 10
- Database :
- Directory of Open Access Journals
- Journal :
- CHIMIA
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.77760779eafd425e854518b6109e1f36
- Document Type :
- article
- Full Text :
- https://doi.org/10.2533/chimia.2017.722