| Affiliation: | 1. Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, Ji'nan, Shandong, 250012 China Shouguang Fukang Pharmaceutical Co., Ltd., 5 xueyuan east street, Shouguang, Shandong, 262799 China;2. Biomedical Science and Technology Industrial Park of Weifang Hi-tech Zone, 36,Gaoxin Second Road, Weifang, Shandong, 261205 China;3. Shouguang Fukang Pharmaceutical Co., Ltd., 5 xueyuan east street, Shouguang, Shandong, 262799 China |
| Abstract: | 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. |
