Melanie Keßler
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View article: Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies Open
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 solubil…
View article: Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies
Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies Open
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 …
View article: Correction to Structure–Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and <i>in Vivo</i> Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers
Correction to Structure–Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and <i>in Vivo</i> Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers Open
Despite the availability of numerous antiepileptic drugs, 20-30% of epileptic patients are pharmacoresistant with seizures not appropriately controlled. Consequently, new strategies to address this unmet medical need are required. T-type c…
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers Open
A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating T-type calcium channel blockers. An optimized derivative, compound 6c, was advanced to in vivo studies, where it demonstrated efficacy in the…
CCDC 1498622: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …