| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10594606 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
The boroProline-based dipeptidyl boronic acids were among the first DPP-IV inhibitors identified, and remain the most potent known. We introduced various substitutions at the 4-position of the boroProline ring regioselectively and stereoselectively, and incorporated these aminoboronic acids into a series of 4-substituted boroPro-based dipeptides. Among these dipeptidyl boronic acids, Arg-(4S)-boroHyp (4q) was the most potent inhibitor of DPP-IV, DPP8 and DPP9, while (4S)-Hyp-(4R)-boroHyp (4o) exhibited the most selectivity for DPP-IV over DPP8 and DPP9.
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Authors
Wengen Wu, Yuxin Liu, Lawrence J. Jr., Ying Shu, Peng Zhao, Youhua Li, Iwona Woznica, Gengli Yu, David G. Sanford, Yuhong Zhou, Sarah E. Poplawski, Beth A. Connolly, James L. Sudmeier, William W. Bachovchin, Jack H. Lai,