Synthesis and drug efficacy validations of racemic-substituted benzimidazoles as antiulcer/antigastric secretion agents

Abstract

Aim: Due to their effective binding affinity to receptors which are responsible for various diseases, benzimidazoles are often bioactive. Present study intended and carried out to synthesis, characterize and develop benzimidazole-based antiulcer drugs. Materials & methods: Established 8a–l were evaluated for gastric antisecretory/antiulcer properties using freshly prepared H+-K+-ATPase from goat fundus mucosa. Molecular docking was carried out to unveil best binding affinities with H+-K+-ATPase (protein data bank ID: 2XZB). Results: The obtained least inhibitory constant of 8a–l (18–92 nM) was comparable to the in vitro H+-K+-ATPase inhibition (IC50: 24–122 nM). Furthermore, the lethal effect of 8a–l to colon cancerous cells and nonharm effect to the normal cells was recognized through cytotoxicity studies. Conclusion: After all in silico, in vitro experimental and structure–activity relationship predictions, the antiulcer druggability potential of 8a–l was recognized. A future drug development study for the most potent compounds among 8a–l is strongly indorsed.