59557-90-3Relevant articles and documents
Synthesis and anti-diabetic activity of novel biphenylsulfonamides as glucagon receptor antagonists
Lee, Chang-Yong,Choi, Hojung,Park, Eun-Young,Nguyen, Thi-Thao-Linh,Maeng, Han-Joo,Mee Lee, Kyoung,Jun, Hee-Sook,Shin, Dongyun
, p. 733 - 750 (2021/08/06)
Type 2 diabetes is characterized by chronic hyperglycemia. Insulin, a hormone secreted from pancreatic β-cells, decreases blood glucose levels, and glucagon, a hormone secreted from pancreatic α-cells, increases blood glucose levels by counterregulation of insulin through stimulation of hepatic glucose production. In diabetic patients, dysregulation of glucagon secretion contributes to hyperglycemia. Thus, inhibition of the glucagon receptor is one strategy for the treatment of hyperglycemia in type 2 diabetes. In this paper, we report a series of biphenylsulfonamide derivatives that were designed, synthesized, and then evaluated by cAMP and hepatic glucose production assays as glucagon receptor antagonists. Of these, compound 7aB-3 decreased glucagon-induced cAMP production and glucagon-induced glucose production in the in vitro assays. Glucagon challenge tests and glucose tolerance tests showed that compound 7aB-3 significantly inhibited glucagon-induced glucose increases and improved glucose tolerance. These results suggest that compound 7aB-3 has therapeutic potential for the treatment of type 2 diabetes.
BIARYL UREA DERIVATIVE OR SALT THEREOF, AND MANUFACTURING AND APPLICATION OF SAME
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Paragraph 0135, (2019/05/10)
The present invention discloses a biaryl urea RORγt inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an RORγt inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an RORγt-related disease.
Orthogonal switching in four-state azobenzene mixed-dimers
Zhao, Fangli,Grubert, Lutz,Hecht, Stefan,Bléger, David
supporting information, p. 3323 - 3326 (2017/03/22)
Azobenzene multi-state switches whose isomerization can be orthogonally induced with photons and electrons are presented. Exposure to green, blue, or ultraviolet light allows toggling between three isomers, while the fourth one is formed selectively via electrocatalytic isomerization.