Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377765 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
Following the discovery of N-acyl-1,4-diazepan-2-one as a novel pharmacophore for potent and selective DPP-4 inhibitors, optimization of this new lead with different substitution on the seven-membered ring resulted in several highly potent and selective, orally bioavailable, and efficacious DPP-4 inhibitors, such as 3R-methyl-1-cyclopropyl-1,4-diazepan-2-one derivative 9i (DPP-4 IC50 = 8.0 nM) and 3R,6R-dimethyl-1,4-diazepan-2-one derivative 14a (DPP-4 IC50 = 9.7 nM).
Graphical abstractPotent, selective, and efficacious DPP-4 inhibitors containing a 1,4-diazepan-2-one moiety were discovered and evaluated.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Gui-Bai Liang, Xiaoxia Qian, Dennis Feng, Tesfaye Biftu, George Eiermann, Huaibing He, Barbara Leiting, Kathy Lyons, Aleksandr Petrov, Ranabir Sinha-Roy, Bei Zhang, Joseph Wu, Xiaoping Zhang, Nancy A. Thornberry, Ann E. Weber,