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

Future Medicinal Chemistry
Rajesh RadhamanalanNarsimaiah Nagaraju

Abstract

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). 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. 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.

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