Synthesis and biological evaluation of novel condensed pyrimidinylmethylsulfinylbenzimidazoles as antiulcer agent

Abstract

Current therapies to treat gastroesophageal reflux disease (GERD), peptic ulcer disease (PUD), and other acid-related diseases either prevent stimulation of the parietal cell (H2-receptor antagonists) or inhibit gastric H+/K+-ATPase (proton pump inhibitors). The inhibition of acid production by proton pump inhibitors (PPI’s) provides more effective relief of symptoms and healing. A series of novel 4-substituted-2-(1H-benzimidazol-2-yl)methylsulfinylpyrimidines were synthesized as target compounds and antiulcer activity was done using parameters like total acidity, pH, and total gastric acid volume by pylorus ligation method on Wistar rats. Three different dose levels were employed for testings. The target compounds 4-substituted-2-(1H-benzimidazol-2-yl)methylsulfinylpyrimidines were effective for ulcer treatment and among them compounds 10c, 10d, 8b, and 8c exhibited potent antisecretory activity. Overall, compounds 10c, 10d, 8b, and 8c can be looked upon as potential leads for further development and investigations.