| Autor: |
Murielle M, Véniant, Clarence, Hale, Randall W, Hungate, Kyung, Gahm, Maurice G, Emery, Janan, Jona, Smriti, Joseph, Jeffrey, Adams, Andrew, Hague, George, Moniz, Jiandong, Zhang, Michael D, Bartberger, Vivian, Li, Rashid, Syed, Steven, Jordan, Renée, Komorowski, Michelle M, Chen, Rod, Cupples, Ki Won, Kim, David J, St Jean, Lars, Johansson, Martin A, Henriksson, Meredith, Williams, Jerk, Vallgårda, Christopher, Fotsch, Minghan, Wang |
| Rok vydání: |
2010 |
| Předmět: |
|
| Zdroj: |
Journal of medicinal chemistry. 53(11) |
| ISSN: |
1520-4804 |
| Popis: |
Thiazolones with an exo-norbornylamine at the 2-position and an isopropyl group on the 5-position are potent 11beta-HSD1 inhibitors. However, the C-5 center was prone to epimerization in vitro and in vivo, forming a less potent diastereomer. A methyl group was added to the C-5 position to eliminate epimerization, leading to the discovery of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). This compound decreased fed blood glucose and insulin levels and reduced body weight in diet-induced obesity mice. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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