| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 5216544 | Tetrahedron | 2014 | 7 Pages |
Abstract
Nobilamide B is a long-acting antagonist of transient receptor potential vanilloid-1 (TRPV1), and is expected to show therapeutic potential for treatment of pain. This linear heptapeptide possesses a Z-didehydroaminobutanoic acid moiety at the C-terminus. Stereoselective construction of the didehydroamino acid moiety was successfully achieved by application of the traceless Staudinger ligation. The combination of solid-phase peptide synthesis and the Staudinger ligation allowed rapid access to not only nobilamide B, but also its macrocyclic analogue nobilamide D.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Tomoya Yamashita, Hiroaki Matoba, Takefumi Kuranaga, Masayuki Inoue,