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Synthesis and 11 beta hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group
- Authors
- 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
- Issue Date
- Jan-2011
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Diabetes; 11beta-HSD1; Thiazolidine; Adamantyl
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.21, no.1, pp.435 - 439
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 21
- Number
- 1
- Start Page
- 435
- End Page
- 439
- ISSN
- 0960-894X
- Abstract
- A new series of thiazolidine derivatives with an adamantyl group was synthesized and evaluated for their ability to inhibit 11 beta-hydroxysteroid dehydrogenase 1 (11 beta-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 11 beta-HSD1, selectivity toward 11 beta-HSD2, metabolic stability, pharmacokinetic, and safety profile. Furthermore, this compound significantly inhibited 11 beta-HSD1 activity in rat and monkey models, and showed improved glycemic control in KKAy mice. (c) 2010 Elsevier Ltd. All rights reserved.
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