3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-Dioxides as ATP-Sensitive Potassium Channel Openers: Effect of 6,7-Disubstitution on Potency and Tissue Selectivity

A series of 6,7-disubstituted 4H-1,2,4-benzothiadiazine 1,1-dioxides bearing a short alkylamino side chain in the 3-position were synthesized. These compounds were tested on rat pancreatic islets and on rat aorta rings. In vitro data indicated that in most cases substitution in the 6 and the 7 posit...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-07, Vol.48 (15), p.4990-5000
Hauptverfasser:	de Tullio, Pascal, Boverie, Stéphane, Becker, Bénédicte, Antoine, Marie-Hélène, Nguyen, Quynh-Anh, Francotte, Pierre, Counerotte, Stéphane, Sebille, Sophie, Pirotte, Bernard, Lebrun, Philippe
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Triphosphate - physiology Animals Aorta - drug effects Aorta - physiology Benzothiadiazines - chemical synthesis Benzothiadiazines - chemistry Benzothiadiazines - pharmacology Biological and medical sciences Cyclic S-Oxides - chemical synthesis Cyclic S-Oxides - chemistry Cyclic S-Oxides - pharmacology General and cellular metabolism. Vitamins In Vitro Techniques Insulin - metabolism Insulin Secretion Ion Channel Gating Islets of Langerhans - drug effects Islets of Langerhans - metabolism Medical sciences Muscle Contraction - drug effects Muscle, Smooth, Vascular - drug effects Muscle, Smooth, Vascular - physiology Organ Specificity Pharmacology. Drug treatments Potassium Channels - drug effects Rats Rats, Wistar Structure-Activity Relationship
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