7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site

[摘要]：Design, synthesis, and SAR of 7-oxopyrrolopyridine-derived DPP4 inhibitors are described. The preferred stereochemistry of these atropisomeric biaryl analogs has been identified as Sa. Compound (+)-3t, with a K(i) against DPP4, DPP8, and DPP9 of 0.37 nM, 2.2, and 5.7 mu M, respectively, showed a significant improvement in insulin response after single doses of 3 and 10 mu mol/kg in ob/ob mice. (C) 2011 Elsevier Ltd. All rights reserved.

[全文传递流程]：

一般上传文献全文的时限在1个工作日内