1587696-68-1Relevant articles and documents
Identification and optimisation of 3,3-dimethyl-azetidin-2-ones as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
McCoull, William,Augustin, Martin,Blake, Caroline,Ertan, Anne,Kilgour, Elaine,Krapp, Stephan,Moore, Jane E.,Newcombe, Nicholas J.,Packer, Martin J.,Rees, Amanda,Revill, John,Scott, James S.,Selmi, Nidhal,Gerhardt, Stefan,Ogg, Derek J.,Steinbacher, Stefan,Whittamore, Paul R. O.
, p. 57 - 63 (2014/01/06)
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.
