A series of 1,2,4-oxadiazol derivatives have been designed and synthesized and 25 compounds were evaluated their abilities by the assay of cAMP concentration in GPR119-transfected HEK293T cells. All compounds showed acceptable agonistic effects on GPR119. Among these compounds, 4p exhibited the best agonistic effects with the EC50 of 20.6nM, which was comparable to that of positive control GPR119 agonist
设计并合成了一系列
1,2,4-恶二唑衍
生物,并通过测定GPR119转染的HEK293T细胞中的c
AMP浓度评估了25种化合物的能力。所有化合物对GPR119显示出可接受的激动作用。在这些化合物中,4p表现出最佳的激动作用,
EC50为20.6nM,与阳性对照GPR119激动剂GSK1292263相当。这些
1,2,4-恶二唑衍
生物的激动活性导致建立结构-活性关系。本文受版权保护。版权所有。