Effect on insulin release of compounds structurally related to the potassium-channel opener 7-chloro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide (BPDZ 73):: introduction of heteroatoms on the 3-alkylamino side chain of the benzothiadiazine 1,1-dioxide ring

被引:12
作者
Boverie, S
Antoine, MH
de Tullio, P
Somers, F
Becker, B
Sebille, S
Lebrun, P
Pirotte, B
机构
[1] Univ Liege, Lab Chim Pharmaceut, B-4000 Liege, Belgium
[2] Free Univ Brussels, Lab Pharmacodynamie & Therapeut, B-1070 Brussels, Belgium
关键词
D O I
10.1211/0022357011776216
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
7-Chloro-3-pyridyl(alkyl)amino-4H-1,2,4-benzothiadiazine 1,1-dioxides and 3-alkylamino-7-chloro-4H-1,2,4-benzothiadiazine 1,1-dioxides containing one or more heteroatoms on the side chain in the 3 position have been synthesized in an attempt to discover new potent K-ATP-channel openers. The compounds were tested as putative pancreatic B-cells K-ATP channel openers by measuring their inhibitory activity on the insulin releasing process. The influence on the biological activity of the nature of the side chain in the 3 position is discussed.
引用
收藏
页码:973 / 980
页数:8
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