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New fluorinated 1,2,4-benzothiadiazine 1,1-dioxides: discovery of an orally active cognitive enhancer acting through potentiation of the 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors.
Francotte P, Goffin E, Fraikin P, Lestage P, Van Heugen JC, Gillotin F, Danober L, Thomas JY, Chiap P, Caignard DH, Pirotte B, de Tullio P. Francotte P, et al. Among authors: danober l. J Med Chem. 2010 Feb 25;53(4):1700-11. doi: 10.1021/jm901495t. J Med Chem. 2010. PMID: 20108934 Free article.
Development of thiophenic analogues of benzothiadiazine dioxides as new powerful potentiators of 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptors.
Francotte P, Goffin E, Fraikin P, Graindorge E, Lestage P, Danober L, Challal S, Rogez N, Nosjean O, Caignard DH, Pirotte B, de Tullio P. Francotte P, et al. Among authors: danober l. J Med Chem. 2013 Oct 24;56(20):7838-50. doi: 10.1021/jm400676g. Epub 2013 Oct 3. J Med Chem. 2013. PMID: 24090223
Synthesis, pharmacological and structural characterization, and thermodynamic aspects of GluA2-positive allosteric modulators with a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide scaffold.
Nørholm AB, Francotte P, Olsen L, Krintel C, Frydenvang K, Goffin E, Challal S, Danober L, Botez-Pop I, Lestage P, Pirotte B, Kastrup JS. Nørholm AB, et al. Among authors: danober l. J Med Chem. 2013 Nov 14;56(21):8736-45. doi: 10.1021/jm4012092. Epub 2013 Nov 5. J Med Chem. 2013. PMID: 24131202
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
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
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
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
31 results