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Design,synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity
Authors:Ahmed OH El-Nezhawy  Ayman R Biuomy  Fatma S Hassan  Ayman K Ismaiel  Hany A Omar
Institution:1. Department of Pharmaceutical Chemistry, College of Pharmacy, Taif University, Saudi Arabia;2. Department of Pharmacology, College of Pharmacy, Taif University, Saudi Arabia;3. Department of Chemistry of Natural and Microbial Products, National Research Center, Dokki, Cairo, Egypt;4. Faculty of Medicine and Medical Sciences, Taif University, Saudi Arabia;5. Pharmacology Department, National Research Center, Dokki, Cairo, Egypt;6. Department of Pharmacology, College of Pharmacy, Beni-Suef University, Egypt
Abstract:A new series of novel benzimidazole derivatives containing substituted pyrid-2-yl moiety and polyhydroxy sugar conjugated to the N-benzimidazole moiety has been synthesized and evaluated as orally bioavailable anti-inflammatory agents with anti-ulcerogenic activity. The anti-inflammatory and anti-ulcerogenic activities of these compounds were compared to diclofenac and omeprazole, respectively. In carrageenan-induced paw oedema assay, 2-methyl-N-((3,4-dimethoxypyridin-2-yl)methyl)-1H-benzimidazol-5-amine (12d) and 1-(1,2,3,5-tetrahydroxy-α-d-mannofuranose)-5-(((3,4-dimethoxypyridin-2yl)methyl)amino)-2-methyl-1H-benzimidazole (15d) displayed dose-dependent anti-inflammatory activities by decreasing the inflammation by 62% and 72%, respectively which is comparable to that of diclofenac (73%). In contrast to diclofenac, the anti-inflammatory activity of these compounds was not only free from any side effects on the gastric mucosa but also showed significant anti-ulcerogenic activity in rat pyloric ligation and ethanol-induced gastric ulcer models similar to that of omeprazole. Together, these findings suggest that 12d and 15d are potent anti-inflammatory agents with concurrent anti-ulcerogenic activity and support its clinical promise as a component of therapeutic strategies for inflammation, for which the gastric side effects are always a major limitation.
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