NDLI: Synthesis and evaluation of succinic acid derivatives as prolyl endopeptidase inhibitors

Content Provider	Springer Nature Link
Author	Lee, Kyung Ho Han, Ah Reum Yoon, Seung Bin Yang, Jae Sung Paik, Young Sook Han, Hyeon Gyu
Copyright Year	2011
Abstract	Many synthetic peptide-based prolyl endopeptidase (PEP) inhibitors are depended on the acy-l-L-prolyl-pyrrolidine structure. The pyrrolidine ring at P1 and a large variety of lipophilic acyl groups at P3 have been reported to be important for potent PEP inhibitory activity. Upon exploration of a new lead compound for PEP inhibition, succinic acid was introduced at the P2 position to replace the l-proline in acyl-l-prolyl-pyrrolidine. A series of amido-succinylpyrrolidine compounds (1–9) were synthesized, and their PEP inhibitory activities were evaluated. Of these, compound 9 showed the most potent PEP inhibitory activity with IC$_{50}$ of 6.4±0.6 nM.
Starting Page	731
Ending Page	737
Page Count	7
File Format	PDF
ISSN	17382203
Journal	Journal of the Korean Society for Applied Biological Chemistry
Volume Number	54
Issue Number	5
e-ISSN	2234344X
Language	English
Publisher	Springer-Verlag
Publisher Date	2011-01-01
Publisher Place	New York
Access Restriction	Subscribed
Subject Keyword	amido-succinyl-pyrrolidine backbone prolyl endopeptidase inhibitor Applied Microbiology Biological Techniques acyl-l-prolyl-pyrrolidine backbone Bioorganic Chemistry
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Biochemistry, Genetics and Molecular Biology

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Synthesis and evaluation of succinic acid derivatives as prolyl endopeptidase inhibitors