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Page 1
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: fraikin 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
In search of novel AMPA potentiators.
Francotte P, de Tullio P, Fraikin P, Counerotte S, Goffin E, Pirotte B. Francotte P, et al. Among authors: fraikin p. Recent Pat CNS Drug Discov. 2006 Nov;1(3):239-46. doi: 10.2174/157488906778773661. Recent Pat CNS Drug Discov. 2006. PMID: 18221205 Review.
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: fraikin p. 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: fraikin p. J Med Chem. 2013 Oct 24;56(20):7838-50. doi: 10.1021/jm400676g. Epub 2013 Oct 3. J Med Chem. 2013. PMID: 24090223
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: fraikin p. J Med Chem. 2014 Nov 26;57(22):9539-53. doi: 10.1021/jm501268r. Epub 2014 Nov 17. J Med Chem. 2014. PMID: 25375781
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: fraikin p. 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
11 results