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Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries.

Publication TypeJournal Article
AuthorsLowe, JT, Lee MD 4th, Akella LB, Davoine E., Donckele EJ, Durak L., Duvall JR, Gerard B., Holson EB, Joliton A., Kesavan S., Lemercier BC, Liu H., Marié JC, Mulrooney CA, Muncipinto G., Welzel-O'Shea M., Panko LM, Rowley A., Suh BC, Thomas M., Wagner FF, Wei J., Foley MA, and Marcaurelle LA
AbstractThe synthesis and diversification of a densely functionalized azetidine ring system to gain access to a wide variety of fused, bridged, and spirocyclic ring systems is described. The in vitro physicochemical and pharmacokinetic properties of representative library members are measured in order to evaluate the use of these scaffolds for the generation of lead-like molecules to be used in targeting the central nervous system. The solid-phase synthesis of a 1976-membered library of spirocyclic azetidines is also described.
Year of Publication2012
JournalThe Journal of organic chemistry
Date Published (YYYY/MM/DD)2012/08/10
ISSN Number0022-3263
DOI10.1021/jo300974j
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/22853001?dopt=Abstract