In:
CHIMIA, Swiss Chemical Society, Vol. 71, No. 10 ( 2017-10-25), p. 722-
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.
Type of Medium:
Online Resource
ISSN:
2673-2424
,
0009-4293
DOI:
10.2533/chimia.2017.722
Language:
Unknown
Publisher:
Swiss Chemical Society
Publication Date:
2017
detail.hit.zdb_id:
2179192-2
