Synthesis and Gastroprotective Evaluation of New Synthetic Indole Imines on Animal Models

Abstract

The present study was designed to carry out the synthesis of targeted N-arylindole imines (derived from 4,5,6-trimethoxy-2,3-diphenyl-1H-indole-7-carbaldehyde), their characterization by spectroscopic and spectrometric methods, and evaluation of gastroprotector activity. The gastroprotective potential of indole imines (5 – 10) was elucidated after peroral administration of compounds in various doses to h EtOH-induced and indomethacin-induced gastric ulcers. In order to determine the mechanism of drug action, the effects of compounds on pH, ulcer index, gastric volume, gastric mucus content, and antioxidant biomarkers were determined. Among five newly synthesized compounds, two halogen derivatives (8 and 9) showed significant protection at 40 and 60 mg/kg doses as compared to standard drug omeprazole. In EtOH-induced gastric ulcer model, indole imine 9 significantly increased the mucus content. Both compounds (8 and 9) were found to attenuate the formation of gastric lesions in indomethacin-induced ulcer model. The serum values of antioxidant biomarkers revealed promising increase in total antioxidant status by compounds 8 and 9. The obtained results suggest the synthetic indole imines 8 and 9 to be remarkable gastroprotective compounds capable of modulating oxidative stress.