Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors
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- 作者：Scott D. Edmondson ; Anthony Mastracchio ; Jason M. Cox ; George J. Eiermann ; Huaibing He ; Kathryn A. Lyons ; Reshma A. Patel ; Sangita B. Patel ; Aleks ; r Petrov ; Giovanna Scapin ; Joseph K. Wu ; Shiyao Xu ; B
- 关键词：Dipeptidyl peptidase-IV ; DPP-4 ; DPP-IV ; Dipeptidyl peptidase 8 ; DPP-8 ; DPP-9 ; Quiescient peptidyl peptidase ; QPP ; GLP-1 ; Glucagon-like peptide 1 ; Benzimidazole ; Imidazopyridine ; Buchwald coupling ; Sitagliptin
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 August 2009
- 年：2009
- 卷：19
- 期：15
- 页码：4097-4101
- 全文大小：410 K
文摘
A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK profiles, and in vivo efficacy of 34 is reported.