✦ LIBER ✦

Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group

✍ Scribed by Sung Wook Kwon; Seung Kyu Kang; Jae Hong Lee; Joo Hwan Bok; Chi Hyun Kim; Sang Dal Rhee; Won Hoon Jung; Hee Youn Kim; Myung Ae Bae; Jin Sook Song; Duck Chan Ha; Hyae Gyoung Cheon; Ki Young Kim; Jin Hee Ahn

Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 882 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.10.123

No coin nor oath required. For personal study only.

✦ Synopsis

A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11b-hydroxysteroid dehydrogenase 1 (11b-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 11b-HSD1, selectivity toward 11b-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11b-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice.

📜 SIMILAR VOLUMES

Discovery of Adamantyl Ethanone Derivati

Discovery of Adamantyl Ethanone Derivatives as Potent 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors

✍ Xiangdong Su; Fabienne Pradaux-Caggiano; Mark P. Thomas; Michelle W. Y. Szeto; H 📂 Article 📅 2010 🏛 John Wiley and Sons 🌐 English ⚖ 858 KB

Adamantyl Ethanone Pyridyl Derivatives:

Adamantyl Ethanone Pyridyl Derivatives: Potent and Selective Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1

✍ Dr. Xiangdong Su; Dr. Fabienne Pradaux-Caggiano; Dr. Nigel Vicker; Dr. Mark P. T 📂 Article 📅 2011 🏛 John Wiley and Sons 🌐 English ⚖ 800 KB

ChemInform Abstract: Identification of C

ChemInform Abstract: Identification of Cyclicsulfonamide Derivatives with an Acetamide Group as 11β-Hydroxysteroid Dehydrogenase 1 Inhibitors.

✍ Jin Hee Ahn; et al. et al. 📂 Article 📅 2011 🏛 John Wiley and Sons ⚖ 41 KB 👁 1 views

## Abstract A series of cyclic sulfonamide derivatives (IX) (31 examples) with an acetamide group in the 2‐position are synthesized and evaluated for their ability to inhibit 11β‐HSD1.