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.
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 KATP-channel openers. The compounds were tested as putative pancreatic B-cells KATP 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.
Boverie
S
S
Laboratoire de Chimie Pharmaceutique, Université de Liège, Belgium.
Antoine
M H
MH
de Tullio
P
P
Somers
F
F
Becker
B
B
Sebille
S
S
Lebrun
P
P
Pirotte
B
B
D000818:Animals; D001581:Benzothiadiazines / Q000737:chemistry / Q000494:pharmacology*; D003981:Diazoxide / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D007328:Insulin / Q000378:metabolism*; D007329:Insulin Antagonists / Q000737:chemistry / Q000494:pharmacology; D000078790:Insulin Secretion; D007515:Islets of Langerhans / Q000187:drug effects* / Q000378:metabolism*; D026902:Potassium Channel Blockers; D051381:Rats; D017208:Rats, Wistar
C416528:7-chloro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide; D001581:Benzothiadiazines; D007328:Insulin; D007329:Insulin Antagonists; D026902:Potassium Channel Blockers; D003981:Diazoxide