Design, Synthesis, Pharmacological Screening and Molecular Docking Study of New Substituted Benzimidazole Derivatives

The present work aimed to study the therapeutic significance of various substituted benzimidazole derivatives in the treatment of peptic ulcers. Aspirin induced gastric ulcer model was used for the study of antiulcer activity using acetyl salicylic acid as ulcer inducing agent and albino rats as the...

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Veröffentlicht in:Pharmaceutical chemistry journal 2023-04, Vol.57 (1), p.51-59
Hauptverfasser: Nalini, C. N., Prabakaran, A., Jayasree, R.
Format: Artikel
Sprache:eng
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Zusammenfassung:The present work aimed to study the therapeutic significance of various substituted benzimidazole derivatives in the treatment of peptic ulcers. Aspirin induced gastric ulcer model was used for the study of antiulcer activity using acetyl salicylic acid as ulcer inducing agent and albino rats as the screening model. Pharmacological screening protocol for the antiulcer activity of synthesized compounds was based on the aspirin induced pylorus ligation method. The synthesized compounds were estimated by determining biochemical parameters such as pH, ulcer index, free acidity and total acidity. The acute oral toxicity studies were performed as per OECD 423 guidelines. The effect of several synthesized substituted benzimidazole compounds were compared to that of the standard drug omeprazole. It was found that compounds R1, R2 and R8 exhibited potent inhibitory activity. The results of molecular docking showed that compound R8 had a maximum binding affinity for H + /K + ATPase of –9.3 kcal/mol. The study revealed that compound R8 has a potent activity and can be used as a lead molecule. Physicochemical properties of synthesized drugs were characterized by spectral techniques.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-023-02850-z