2. Academic Validation
  3. Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group

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

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):435-9. doi: 10.1016/j.bmcl.2010.10.123.
Sung Wook Kwon 1,  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
Affiliations

Affiliation

  • 1 Department of Chemistry, Korea University, Seoul 136-701, Republic of Korea.
PMID: 21093259 DOI: 10.1016/j.bmcl.2010.10.123
Abstract

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.

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