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ORIGINAL ARTICLE
Year : 2013  |  Volume : 5  |  Issue : 1  |  Page : 39-43

Synthesis and PASS-assisted in silico approach of some novel 2-substituted benzimidazole bearing a pyrimidine-2, 4, 6(trione) system as mucomembranous protector


1 Department of Pharmaceutical Chemistry, Grace College of Pharmacy, Palakkad, Kerala, India
2 Department of Pharmaceutical Chemistry, Madras Medical College, Chennai, Tamil Nadu, India
3 Department of Pharmaceutical Chemistry, Karuna College of Pharmacy, Palakkad, Kerala, India

Correspondence Address:
Bijo Mathew
Department of Pharmaceutical Chemistry, Grace College of Pharmacy, Palakkad, Kerala
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0975-7406.106563

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Purpose: The present paper demonstrates the utility of PASS computer-aided program and makes a clear comparison of predicted and observed pharmacological properties of some novel 5-[(2E)-1-(1H-benzimidazol-2-yl)-3-substituted phenylprop-2-en-1-ylidene] pyrimidine-2, 4, 6 (1H, 3H, 5H)-triones (5a-f). Materials and Methods: The synthesis of the titled derivatives were achieved by the reaction between 2E)-1-(1H-benzimidazol-2-yl)-3-phenylprop-2-en-1-ones (4a-f) and barbituric acid in the presence of catalytic amount of acetic acid medium. All the final structures were assigned on the basis of IR, 1 HNMR and mass spectra analysis. All the newly synthesized compounds were screened for their antiulcer activity in the pylorus-ligated rats. Results: Compounds 5b, 5e and 5c showed a percentage protection of (69.58, 69.56 and 67.17 at a dose of 50 mg/kg b.w.) when compared to standard omeprazole (77.37%, 2 mg/kg b.w.). Conclusion: Scanning of stomach specimens using electron microscope revealed that the mice treated with standard and synthetic derivatives had no injury observed in stomach mucosa, which is identical to that of the control animal.


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