Synthesis of novel Diazaspirodecanones as potential GPa inhibitors
MetadataShow full item record
Glycogen Phosphorylase (GP) is a therapeutic target for treating hyperglycemia and binds to the C-terminus (residues 269-284; PEWPSYLGYEKLGPYY) of the hepatic glycogen-binding (GL)-subunit of protein phophatase-1 (PP-1). In a de novo approach, a unique section within the C-terminus sequence was identified. 1,7-diazaspiro[4.5]decan-6-one 1 was selected as a scaffold for lead compd. identification. Reported 1,7-diazaspiro[4.5]decan-6-ones are either N1-functionalised or exist as tricyclic spirolactams. The novel synthesis of a C8-substituted spiro scaffold is presented.
Abstracts of Papers, 239th ACS National Meeting, San Francisco, CA, United States, March 21-25, 2010 (2010)
Organic Chemical Synthesis