Bibia Heidmann
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View article: Front Cover: The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders (ChemMedChem 23/2020)
Front Cover: The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders (ChemMedChem 23/2020) Open
The Front Cover illustrates a circadian rhythm accompanied by daridorexant, Idorsia′s dual orexin receptor antagonist (DORA), investigated for the treatment of insomnia. It represents the quest for a DORA that would provide the next-day be…
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: ACT-451840 blocking transmission.
ACT-451840 blocking transmission. Open
Standard membrane feeding assays were performed with a 24 h pre-incubation of gametocytes with compound (indirect mode). (A) shows average oocyst intensity per mosquito and (B) shows average oocyst prevalence (percentage of mosquitoes with…
View article: Parasite Reduction Ratio.
Parasite Reduction Ratio. Open
The number of viable P. falciparum strain 3D7 (MR4) versus treatment time is compared between ACT-451840 and a selection of standard antimalarials (data for the latter was previously reported in reference [24]). Data are the mean ± SD of f…
View article: Antimalarial activity in <i>P</i>. <i>berghei</i> infected mice plotted against AUC, C<sub>max</sub>, and time above threshold over the entire treatment period (1 or 3 d).
Antimalarial activity in <i>P</i>. <i>berghei</i> infected mice plotted against AUC, C<sub>max</sub>, and time above threshold over the entire treatment period (1 or 3 d). Open
Dots are the observed antimalarial activity; the line is the modeled relationship using a maximal effect (Emax) model.
View article: Cover Picture: Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold‐Hopping Approach (ChemMedChem 19/2016)
Cover Picture: Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold‐Hopping Approach (ChemMedChem 19/2016) Open
The front cover picture shows the successful application of a scaffold-hopping approach starting from the upper model structure and replacing the central core with different bicyclic diamine templates (some representative templates are dep…
View article: Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling
Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling Open
Background Artemisinin resistance observed in Southeast Asia threatens the continued use of artemisinin-based combination therapy in endemic countries. Additionally, the diversity of chemical mode of action in the global portfolio of marke…
View article: Back Cover: Discovery and Characterization of ACT‐451840: an Antimalarial Drug with a Novel Mechanism of Action (ChemMedChem 18/2016)
Back Cover: Discovery and Characterization of ACT‐451840: an Antimalarial Drug with a Novel Mechanism of Action (ChemMedChem 18/2016) Open
The back cover picture shows the successful collaboration between the Swiss TPH and Actelion Pharmaceuticals Ltd from the phenotypic screening hit via animal experiments to the antimalarial clinical candidate ACT-451840, exhibiting a novel…