Olivier Bezencon
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Explore the profile of Olivier Bezencon including associated specialties, affiliations and a list of published articles.
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Articles
13
Citations
38
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Recent Articles
1.
Surivet J, Jacob E, Kessler M, Kohl C, Vaillant C, Bezencon O, et al.
Bioorg Med Chem
. 2025 Mar;
122:118132.
PMID: 40048842
We describe the optimization of 2-acyl-1-biarylmethylpyrazolidines, a novel class of dual orexin receptor antagonists (DORAs) designed for the treatment of sleep disorders requiring a rapid onset (<30 min) and a...
2.
Surivet J, Kessler M, Vaillant C, Aissaoui H, Bezencon O, Busch L, et al.
Bioorg Med Chem
. 2024 Sep;
112:117892.
PMID: 39236468
Dual orexin receptor antagonists (DORAs) are approved for the treatment of sleep onset and/or sleep maintenance insomnia. In the present disclosure, we report the discovery of a new class of...
3.
Bezencon O, Heidmann B, Siegrist R, Stamm S, Richard S, Pozzi D, et al.
J Med Chem
. 2017 Nov;
60(23):9769-9789.
PMID: 29116786
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...
4.
Bezencon O, Remen L, Richard S, Roch C, Kessler M, Ertel E, et al.
Bioorg Med Chem Lett
. 2017 Oct;
27(23):5326-5331.
PMID: 29074257
We identified and characterized a series of pyrrole amides as potent, selective Ca3.2-blockers. This series culminated with the identification of pyrrole amides 13b and 26d, with excellent potencies and/or selectivities...
5.
Bezencon O, Siegrist R, Heidmann B, Pozzi D, Stamm S, Remen L, et al.
Chimia (Aarau)
. 2017 Oct;
71(10):722-729.
PMID: 29070417
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...
6.
Bezencon O, Remen L, Richard S, Roch C, Kessler M, Moon R, et al.
Bioorg Med Chem Lett
. 2017 Oct;
27(23):5322-5325.
PMID: 29066309
We identified and characterized a series of pyrazole amides as potent, selective Ca3.1-blockers. This series culminated with the identification of pyrazole amides 5a and 12d, with excellent potencies and/or selectivities...
7.
Siegrist R, Pozzi D, Jacob G, Torrisi C, Colas K, Braibant B, et al.
J Med Chem
. 2017 Feb;
60(5):2163.
PMID: 28234473
No abstract available.
8.
Siegrist R, Pozzi D, Jacob G, Torrisi C, Colas K, Braibant B, et al.
J Med Chem
. 2016 Dec;
59(23):10661-10675.
PMID: 27933950
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...
9.
Remen L, Bezencon O, Simons L, Gaston R, Downing D, Gatfield J, et al.
J Med Chem
. 2016 Sep;
59(18):8398-411.
PMID: 27579577
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...
10.
Corminboeuf O, Bezencon O, Remen L, Grisostomi C, Richard-Bildstein S, Bur D, et al.
Bioorg Med Chem Lett
. 2010 Sep;
20(21):6291-6.
PMID: 20843690
The optimization of the 4-position of recently described new 3,4-disubstituted piperidine-based renin inhibitors is reported herein. The synthesis and characterization of compounds leading to the discovery of 11 (ACT-178882, MK-1597),...