1346555-34-7Relevant articles and documents
Synthesis and biological evaluation of picolinamides as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
Ryu, Je Ho,Kim, Shinae,Han, Hye Young,Son, Hyun Joo,Lee, Hyun Jung,Shin, Young Ah,Kim, Jae-Sun,Park, Hyeung-Geun
, p. 695 - 700 (2015/01/30)
Synthesis of a series of 6-substituted picolinamide derivatives and their inhibitory activities against 11β-hydroxysteroid dehydrogenase type 1 are described. Optimization of the initial hit compound, N-cyclohexyl-6-(piperidin-1-yl)picolinamide (1) from high throughput screening of in-house library resulted in the discovery of the highly potent and metabolically stable compound 25, which was efficacious in a mouse ex vivo pharmacodynamic model and reduced the fasting blood glucose and insulin levels in a HF/STZ mouse model after oral dosing.