Design, Synthesis, and Preliminary Activity Evaluation of Novel Pyrimidine Derivatives as Acid Pump Antagonists

作者：Song Weiguo; Zhang Xiaopan; Li Shutao; Xu Wenfang^*

来源：Chemical Biology & Drug Design, 2015, 85(3): 306-314.

DOI：10.1111/cbdd.12390

• acid pump antagonists
• bioisosterism
• gastric antisecretory activity
• pyrimidine derivatives
• synthesis

Acid-related diseases of the upper gastrointestinal tract, especially gastroesophageal reflux disease (GERD), remain a widespread problem worldwide. In this paper, we reported the design, synthesis, and preliminary gastric antisecretory activity evaluation of novel pyrimidine derivatives as acid pump antagonists. The gastric antisecretory activity assay results showed that all compounds displayed potent gastric antisecretory activity when gastric secretion was stimulated by histamine. The most potent compound 5g exhibited even similar gastric antisecretory activity compared with the control revaprazan, and the relative inhibition rate was 93.0%, which was worthy of further investigation.

• 出版日期2015-3
• 单位山东大学