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Identification and optimisation of 3,3-dimethyl-azetidin-2-ones as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
- Source :
- Med. Chem. Commun.. 5:57-63
- Publication Year :
- 2014
- Publisher :
- Royal Society of Chemistry (RSC), 2014.
-
Abstract
- 3,3-Di-methyl-azetidin-2-ones were identified as potent and selective 11β-HSD1 inhibitors against the human and mouse forms of the enzyme. Structure guided optimisation of LLE was conducted, utilising a key polar interaction and identifying stereochemical preference for the 4S isomer. Metabolic stability was improved to afford oral exposure, providing tool compounds suitable for pre-clinical evaluation.
Details
- ISSN :
- 20402511 and 20402503
- Volume :
- 5
- Database :
- OpenAIRE
- Journal :
- Med. Chem. Commun.
- Accession number :
- edsair.doi...........d5ec1d9e811431313f5ae29a9b1caaaf