Discovery of a Potent, Selective T‑type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies

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 m...

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Veröffentlicht in:	Journal of medicinal chemistry 2017-12, Vol.60 (23), p.9769-9789
Hauptverfasser:	Bezençon, 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
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzeneacetamides - chemistry Benzeneacetamides - metabolism Benzeneacetamides - pharmacokinetics Benzeneacetamides - pharmacology Brain - drug effects Brain - metabolism Calcium Channel Blockers - chemistry Calcium Channel Blockers - metabolism Calcium Channel Blockers - pharmacokinetics Calcium Channel Blockers - pharmacology Calcium Channels, T-Type - metabolism Dogs Drug Discovery Epilepsy, Generalized - drug therapy Epilepsy, Generalized - metabolism Guinea Pigs Humans Macaca fascicularis Pyrazoles - chemistry Pyrazoles - pharmacology Rats, Wistar Structure-Activity Relationship
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