Han Bei, Huan Yi, Lin Zi-Yun, Li Peng, Shen Zhu-Fang, Yin Da-Li, Huang Hai-Hong
Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China.
Yao Xue Xue Bao. 2010 Nov;45(11):1379-84.
To research the structure-activity relationship (SAR) of glycinamide-bearing compounds that used as inhibitors of dipeptidyl peptidase IV (DPP-IV), P32/98 and compound A were chosen as the leading compounds, heterocycles containing nitrogen atom were introduced to form amide, and different residues on a-position of carbonyl were designed. The nineteen designed compounds were synthesized by a simple route and were evaluated as inhibitors of DPP-IV. All of the structures were characterized by 1H NMR and HRMS. The preliminary SAR result was obtained.
为研究用作二肽基肽酶IV（DPP-IV）抑制剂的含甘氨酰胺化合物的构效关系（SAR），选择P32/98和化合物A作为先导化合物，引入含氮杂环形成酰胺，并设计羰基α位的不同取代基。通过简单路线合成了19个设计化合物，并对其作为DPP-IV抑制剂进行了评估。所有结构均通过1H NMR和HRMS进行了表征。获得了初步的构效关系结果。
