950606-92-5Relevant academic research and scientific papers
Discovery and biological evaluation of potent and orally active human 11β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes mellitus
Koike, Takanori,Shiraki, Ryota,Sasuga, Daisuke,Hosaka, Mitsuru,Kawano, Tomoaki,Fukudome, Hiroki,Kurosawa, Kazuo,Moritomo, Ayako,Mimasu, Shinya,Ishii, Hirofumi,Yoshimura, Seiji
, p. 824 - 838 (2019)
We synthesized and evaluated novel 5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole derivatives as 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors. Optimization of the thiophene ring and the substituents on the 1,2,4-triazole ring produced
TRIAZOLE DERIVATIVE OR SALT THEREOF
-
Page/Page column 29; 63; 89, (2009/01/20)
[Problem] To provide a compound which may be used in treating diseases in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, especially diabetes and insulin resistance. [Means for Solution] It was found that a triazole derivative or a pharmaceutically acceptable salt thereof, in which the 3-position of triazole ring is substituted with a trisubstituted methyl group and the 5-position is substituted with a lower alkyl, cycloalkyl or the like, has a strong 11β-HSD1-inhibitory activity. In addition, since the triazole derivative of the present invention shows excellent blood glucose-lowering action, it may be used in the treatment of diabetes and insulin resistance.
