1265898-47-2Relevant academic research and scientific papers
Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group
Kwon, Sung Wook,Kang, Seung Kyu,Lee, Jae Hong,Bok, Joo Hwan,Kim, Chi Hyun,Rhee, Sang Dal,Jung, Won Hoon,Kim, Hee Youn,Bae, Myung Ae,Song, Jin Sook,Ha, Duck Chan,Cheon, Hyae Gyoung,Kim, Ki Young,Ahn, Jin Hee
supporting information; experimental part, p. 435 - 439 (2011/02/28)
A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1). Our initial compound 5a showed a weak inhibitory activity. Significant improvements in potency were achieved by substituent modification. The potent compound 8g (E) showed good in vitro inhibitory activity toward human 11β-HSD1, selectivity toward 11β-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11β-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice.
