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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: pirotte b. J Med Chem. 2014 Nov 26;57(22):9539-53. doi: 10.1021/jm501268r. Epub 2014 Nov 17. J Med Chem. 2014. PMID: 25375781
3-and 4-substituted 4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as potassium channel openers: synthesis, pharmacological evaluation, and structure-activity relationships.
de Tullio P, Pirotte B, Lebrun P, Fontaine J, Dupont L, Antoine MH, Ouedraogo R, Khelili S, Maggetto C, Masereel B, Diouf O, Podona T, Delarge J. de Tullio P, et al. Among authors: pirotte b. J Med Chem. 1996 Feb 16;39(4):937-48. doi: 10.1021/jm9500582. J Med Chem. 1996. PMID: 8632417
Esters and amides of 6-(chloromethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid as inhibitors of alpha-chymotrypsin: significance of the "aromatic" nature of the novel ester-type coumarin for strong inhibitory activity.
Pochet L, Doucet C, Schynts M, Thierry N, Boggetto N, Pirotte B, Jiang KY, Masereel B, de Tullio P, Delarge J, Reboud-Ravaux M. Pochet L, et al. Among authors: pirotte b. J Med Chem. 1996 Jun 21;39(13):2579-85. doi: 10.1021/jm960090b. J Med Chem. 1996. PMID: 8691456
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors: design, synthesis, pharmacology, and structure-activity relationships.
Pirotte B, Podona T, Diouf O, de Tullio P, Lebrun P, Dupont L, Somers F, Delarge J, Morain P, Lestage P, Lepagnol J, Spedding M. Pirotte B, et al. J Med Chem. 1998 Jul 30;41(16):2946-59. doi: 10.1021/jm970694v. J Med Chem. 1998. PMID: 9685234
Preparation and pharmacological evaluation of the R- and S-enantiomers of 3-(2-butylamino)-4H- and 3-(3-methyl-2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide, two tissue selective ATP-sensitive potassium channel openers.
Khelili S, de Tullio P, Lebrun P, Fillet M, Antoine MH, Ouedraogo R, Dupont L, Fontaine J, Felekidis A, Leclerc G, Delarge J, Pirotte B. Khelili S, et al. Among authors: pirotte b. Bioorg Med Chem. 1999 Aug;7(8):1513-20. doi: 10.1016/s0968-0896(99)00082-6. Bioorg Med Chem. 1999. PMID: 10482443
251 results