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Design, Synthesis, and Preliminary Activity Evaluation of Novel Pyrimidine Derivatives as Acid Pump Antagonists
Author(s) -
Song Weiguo,
Zhang Xiaopan,
Li Shutao,
Xu Wenfang
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12390
Subject(s) - gastric acid , pyrimidine , histamine , gerd , reflux , secretion , chemistry , pharmacology , histamine antagonists , medicine , biochemistry , disease
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.