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.
Supplementary data
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Financial and competing interests disclosure
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
No writing assistance was utilized in the production of this manuscript.
Ethical conduct of interest
Declared none.