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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: francotte p. 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
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: francotte p. 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
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: francotte p. 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
7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency.
Goffin E, Drapier T, Larsen AP, Geubelle P, Ptak CP, Laulumaa S, Rovinskaja K, Gilissen J, Tullio P, Olsen L, Frydenvang K, Pirotte B, Hanson J, Oswald RE, Kastrup JS, Francotte P. Goffin E, et al. Among authors: francotte p. J Med Chem. 2018 Jan 11;61(1):251-264. doi: 10.1021/acs.jmedchem.7b01323. Epub 2017 Dec 19. J Med Chem. 2018. PMID: 29256599 Free PMC article.
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. 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.
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