Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor

Autor: Valerie Brault, Sonia Bernetiere, José Camara, Pascale Plas, Pierre Roubert, Lydie Poitout, Carole Sackur

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:4464-4470

A novel series of benzimidazoles was identified and optimized, leading to the discovery of potent and selective antagonists of the human melanocortin-4 receptor. In addition, compound 5i was shown to cross the blood-brain barrier after intravenous do

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd422ef705bb9e0089e5f9af72d36fe1
https://doi.org/10.1016/j.bmcl.2007.06.010

Novel non-peptide ligands for the somatostatin sst3 receptor

Autor: Lydie Poitout, Marie-Odile Contour-Galcera, Barry A. Morgan, Christophe Moinet, Pierre Roubert, Thomas D. Gordon, Christophe Thurieau

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 11:991-995

A series of imidazole derivatives has been prepared using high throughput parallel synthesis. Several compounds showed high affinity (Ki in 10(-6)-10(-8) M range) and selectivity at recombinant human somatostatin receptor subtype 3 (hsst3).

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6db752c43d5af47bfe645113bd87d6c2
https://doi.org/10.1016/s0960-894x(01)00107-x

Synthesis of azasugars as potent inhibitors of glycosidases

Autor: Isabelle Dosbaa, Yves Le Merrer, Jean-Claude Depezay, Marie-José Foglietti, Sabine Geoffroy, Lydie Poitout

Publikováno v: Bioorganic & Medicinal Chemistry. 5:519-533

A series of enantiomerically pure azasugars (2,5-dideoxy-2,5-imino- d -mannitol, 1-deoxynojirimycin, 1-deoxymannojirimycin, and related compounds) was synthesized from d -mannitol via aminoheterocyclization of C 2 -symmetric bis-epoxides and subseque

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::694f54afe983d8967230b252943d1c54
https://doi.org/10.1016/s0968-0896(96)00266-0

Synthesis of azasugars. Part 1 isomerization of polyhydroxylated piperidines

Autor: Jean-Claude Depezay, Yves Le Merrer, Lydie Poitout

Publikováno v: Tetrahedron Letters. 37:1609-1612

N- Benzyl -3,4- di -O- benzyl-1,5-dideoxy-1,5-imino- d -glucitol and l -gulitol undergo easy isomerization, mainly either by ring contraction, or either by SN 2 inversion at C2. This isomerization performed by bis-hydroxyl activation allows to access

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0238569dc5402e88de9827f1e930dd3e
https://doi.org/10.1016/0040-4039(96)00096-2

M4 Safety and tolerability of BN82451B in huntington’s disease

Autor: S. Bohlen, Klaus Seppi, Adolf Weindl, Alzbeta Mühlbäck, Stephan Klebe, Alexander Storch, Matthias Löhle, Katrin Reetz, Ingo Meyer, Thomas Klopstock, Zacharias Kohl, Johannes Schiefer, Christian Saß, Robin Schubert, Lydie Poitout, Ralf Reilmann, Ludger Schöls, Werner Rein, Alexander Münchau, Ralf Marquard, Frank Schaumann, Carsten Saft, Raphael M. Bonelli, Carine Brisset, Isabelle Paty, Kai Boelmans

Publikováno v: Journal of neurology, neurosurgery, and psychiatry 87(Suppl 1), A102.2-A103 (2016). doi:10.1136/jnnp-2016-314597.289
9th Plenary Meeting 2016 European Huntington's Disease Network, The Hague, The Netherlands, 2016-09-16-2016-09-18

Background BN82451B is a small, orally active molecule with good CNS penetration. Preclinical studies in tgHD R6/2 mice suggested improved motor function and prolonged survival. In addition antidyskinetic activity was observed in other models. The pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc2ab56dd403c9ec2c225f140fae9477
https://doi.org/10.1136/jnnp-2016-314597.289