3N-methylbiphenylsulfonylurea and -carbamate substituted imidazo[4,5-b]pyridines. Potent antagonists of the ANG II AT1 receptors.
The synthesis and the SAR study of imidazo[4,5-b]pyridine biphenyl sulfonylureas and -carbamates as highly potent AT1-selective ANG II receptor antagonists are described. Several members of this new class of antagonists efficiently inhibited the ANG II-induced pressor response in pithed rats after iv and intraduodenal (id) administration.
Heitsch
H
H
Hoechst AG, Frankfurt/Main, Germany.
Becker
R H
RH
Kleemann
H W
HW
Wagner
A
A
D000804:Angiotensin II / Q000037:antagonists & inhibitors*; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D002219:Carbamates / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003655:Decerebrate State; D004386:Duodenum / Q000378:metabolism; D066298:In Vitro Techniques; D007275:Injections, Intravenous; D007928:Lethal Dose 50; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D051381:Rats; D013329:Structure-Activity Relationship; D013453:Sulfonylurea Compounds / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D057911:Angiotensin Receptor Antagonists; D002219:Carbamates; D013453:Sulfonylurea Compounds; D000804:Angiotensin II