Toward Tissue-Selective Pancreatic B-Cells KATP Channel Openers Belonging to 3-Alkylamino-7-halo-4 H-1, 2, 4-benzothiadiazine 1, 1-Dioxides

…, P Wahl, MH Antoine, F Somers, S Sebille…

文献索引：De Tullio, Pascal; Becker, Benedicte; Boverie, Stephane; Dabrowski, Michael; Wahl, Philip; Antoine, Marie-Helene; Somers, Fabian; Sebille, Sophie; Ouedraogo, Raogo; Hansen, John Bondo; Lebrun, Philippe; Pirotte, Bernard Journal of Medicinal Chemistry, 2003 , vol. 46, # 15 p. 3342 - 3353

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被引用次数: 49

摘要

3-(Alkylamino)-7-halo-4 H-1, 2, 4-benzothiadiazine 1, 1-dioxides were synthesized, and their activity on rat-insulin-secreting cells and rat aorta rings was compared to that of the KATP channel activators diazoxide and pinacidil. Structure-activity relationships indicated that an improved potency and selectivity for the pancreatic tissue was obtained by introducing a fluorine atom in the 7-position and a short linear (preferably ethyl) or cyclic ( ...