The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 6-(Piperazin-1-yl)nicotinonitrile( cas:149554-29-0 ) is researched.Formula: C10H12N4.Ryu, Je Ho; Kim, Shinae; Lee, Jung A.; Han, Hye Young; Son, Hyun Joo; Lee, Hyun Jung; Kim, Yong Hyuk; Kim, Jae-Sun; Park, Hyeung-geun published the article 《Synthesis and optimization of picolinamide derivatives as a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors》 about this compound( cas:149554-29-0 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: picolinamide derivative synthesis optimization hydroxysteroid dehydrogenase inhibitor; 11β-HSD1 inhibitor; Diabetes; Hyperlipidemia; Metabolic syndrome; Picolinamide. Let’s learn more about this compound (cas:149554-29-0).
The synthesis and structure-activity relationship of a series of 6-substituted picolinamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1 are described. The optimization of the left-hand side of lead compound I resulted in the discovery of the highly potent, selective, and orally available inhibitor II, which demonstrated an excellent activity in a mouse ex vivo pharmacodynamic model. Moreover, II reduced the blood glucose and improved the lipid profiles in ob/ob mice after oral administration.
《Synthesis and optimization of picolinamide derivatives as a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(6-(Piperazin-1-yl)nicotinonitrile)Formula: C10H12N4.
Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI