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New insights in the development of positive allosteric modulators of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors belonging to 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides: Introduction of (mono/difluoro)methyl groups at the 2-position of the thiadiazine ring.
Goffin E, Fraikin P, Abboud D, de Tullio P, Beaufour C, Botez I, Hanson J, Danober L, Francotte P, Pirotte B. Goffin E, et al. Among authors: danober l. Eur J Med Chem. 2023 Mar 15;250:115221. doi: 10.1016/j.ejmech.2023.115221. Epub 2023 Feb 24. Eur J Med Chem. 2023. PMID: 36863228
Exploring thienothiadiazine dioxides as isosteric analogues of benzo- and pyridothiadiazine dioxides in the search of new AMPA and kainate receptor positive allosteric modulators.
Francotte P, Bay Y, Goffin E, Colson T, Lesenfants C, Dorosz J, Laulumaa S, Fraikin P, de Tullio P, Beaufour C, Botez I, Pickering DS, Frydenvang K, Danober L, Kristensen AS, Kastrup JS, Pirotte B. Francotte P, et al. Among authors: danober l. Eur J Med Chem. 2024 Jan 15;264:116036. doi: 10.1016/j.ejmech.2023.116036. Epub 2023 Dec 9. Eur J Med Chem. 2024. PMID: 38101041 Free article.
Development of Thiochroman Dioxide Analogues of Benzothiadiazine Dioxides as New Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors.
Etsè KS, Dorosz J, McLain Christensen K, Thomas JY, Botez Pop I, Goffin E, Colson T, Lestage P, Danober L, Pirotte B, Kastrup JS, Francotte P. Etsè KS, et al. Among authors: danober l. ACS Chem Neurosci. 2021 Jul 21;12(14):2679-2692. doi: 10.1021/acschemneuro.1c00255. Epub 2021 Jul 9. ACS Chem Neurosci. 2021. PMID: 34242002
Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors.
Bretin S, Louis C, Seguin L, Wagner S, Thomas JY, Challal S, Rogez N, Albinet K, Iop F, Villain N, Bertrand S, Krazem A, Bérachochéa D, Billiald S, Tordjman C, Cordi A, Bertrand D, Lestage P, Danober L. Bretin S, et al. Among authors: danober l. PLoS One. 2017 Sep 8;12(9):e0184429. doi: 10.1371/journal.pone.0184429. eCollection 2017. PLoS One. 2017. PMID: 28886144 Free PMC article.
In vivo pharmacological profile of S 38093, a novel histamine H3 receptor inverse agonist.
Panayi F, Sors A, Bert L, Martin B, Rollin-Jego G, Billiras R, Carrié I, Albinet K, Danober L, Rogez N, Thomas JY, Pira L, Bertaina-Anglade V, Lestage P. Panayi F, et al. Among authors: danober l. Eur J Pharmacol. 2017 May 15;803:1-10. doi: 10.1016/j.ejphar.2017.03.008. Epub 2017 Mar 14. Eur J Pharmacol. 2017. PMID: 28315340
Synthesis and Pharmacology of Mono-, Di-, and Trialkyl-Substituted 7-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides Combined with X-ray Structure Analysis to Understand the Unexpected Structure-Activity Relationship at AMPA Receptors.
Larsen AP, Francotte P, Frydenvang K, Tapken D, Goffin E, Fraikin P, Caignard DH, Lestage P, Danober L, Pirotte B, Kastrup JS. Larsen AP, et al. Among authors: danober l. ACS Chem Neurosci. 2016 Mar 16;7(3):378-90. doi: 10.1021/acschemneuro.5b00318. Epub 2016 Feb 1. ACS Chem Neurosci. 2016. PMID: 26771108
Thermodynamic characterization of new positive allosteric modulators binding to the glutamate receptor A2 ligand-binding domain: combining experimental and computational methods unravels differences in driving forces.
Nørholm AB, Francotte P, Goffin E, Botez I, Danober L, Lestage P, Pirotte B, Kastrup JS, Olsen L, Oostenbrink C. Nørholm AB, et al. Among authors: danober l. J Chem Inf Model. 2014 Dec 22;54(12):3404-16. doi: 10.1021/ci500559b. Epub 2014 Dec 9. J Chem Inf Model. 2014. PMID: 25420075
Positive allosteric modulators of 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors belonging to 4-cyclopropyl-3,4-dihydro-2h-1,2,4-pyridothiadiazine dioxides and diversely chloro-substituted 4-cyclopropyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides.
Francotte P, Nørholm AB, Deva T, Olsen L, Frydenvang K, Goffin E, Fraikin P, de Tullio P, Challal S, Thomas JY, Iop F, Louis C, Botez-Pop I, Lestage P, Danober L, Kastrup JS, Pirotte B. Francotte P, et al. Among authors: danober l. J Med Chem. 2014 Nov 26;57(22):9539-53. doi: 10.1021/jm501268r. Epub 2014 Nov 17. J Med Chem. 2014. PMID: 25375781
31 results