Journal of Medicinal Chemistry p. 9769 - 9789 (2017)
Update date:2022-08-15
Topics:
Bezen?on, Olivier
Heidmann, Bibia
Siegrist, Romain
Stamm, Simon
Richard, Sylvia
Pozzi, Davide
Corminboeuf, Olivier
Roch, Catherine
Kessler, Melanie
Ertel, Eric A.
Reymond, Isabelle
Pfeifer, Thomas
De Kanter, Ruben
Toeroek-Schafroth, Michael
Moccia, Luca G.
Mawet, Jacques
Moon, Richard
Rey, Markus
Capeleto, Bruno
Fournier, Elvire
We report here the discovery and pharmacological characterization of N-(1-benzyl-1H-pyrazol-3-yl)-2-phenylacetamide derivatives as potent, selective, brain-penetrating T-type calcium channel blockers. Optimization focused mainly on solubility, brain penetration, and the search for an aminopyrazole metabolite that would be negative in an Ames test. This resulted in the preparation and complete characterization of compound 66b (ACT-709478), which has been selected as a clinical candidate.
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