Identification and optimisation of 3,3-dimethyl-azetidin-2-ones as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) was written by 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.. And the article was included in MedChemComm in 2014.Reference of 141234-08-4 This article mentions the following:
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 optimization of LLE was conducted, utilizing a key polar interaction and identifying stereochem. preference for the 4S isomer. Metabolic stability was improved to afford oral exposure, providing tool compounds suitable for pre-clin. evaluation. In the experiment, the researchers used many compounds, for example, Quinoxaline-5-carbaldehyde (cas: 141234-08-4Reference of 141234-08-4).
Quinoxaline-5-carbaldehyde (cas: 141234-08-4) belongs to quinoxaline derivatives. Quinoxaline derivatives are important constituents of pharmacologically active compounds, including as well as for RNA synthesis inhibition, reactive dyes and pigments, azo dyes, flurox Cylin Dyes, Corrosion Inhibitors and Photovoltaic Polymers. Quinoxalines are used in the treatment of bacterial, cancer, and HIV infections. Moreover, varenicline, a clinical drug is used for treating nicotine addiction, also contains quinoxaline moiety.Reference of 141234-08-4
Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider