Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity |
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Authors: | Fatmah A.S. Alasmary Amani S. Awaad Ahmed M. Alafeefy Reham M. El-Meligy Saleh I. Alqasoumi |
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Affiliation: | 1. Chemistry Department, College of Science, King Saud University, Riyadh 11362, Saudi Arabia;2. Pharmacognosy Department, College of Pharmacy, Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia;3. Department of Chemistry, Kulliyyah of Science, International Islamic University Malaysia, Malaysia;4. Aromatic and Medicinal Plants Department, Desert Research Center, Cairo, Egypt;5. Department of Pharmacognosy, College of Pharmacy, King Saud University, KSA |
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Abstract: | Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl-3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4-aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & Anti-Ulcerative colitis activities.All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The effect of the tested compounds 5, 6 & 11 at dose 50?mg/kg were significantly (P < 0.01) more effective than dexamesathone (0.1?mg/kg) in reducing all parameters.Compounds showed curative activity of for peptic ulcer (induced by absolute alcohol (at a dose of 50?mg/kg, it produced Curative of control ulcer 56.00%, 61.70% & 87.1% for compounds 5, 6 & 11 respectively at dose 50?mg/kg, while the standard drug (Omeprazole 20?mg/kg) produced 33.3%. In both tests, the activity of our target compounds were higher than the standard drugs used for treatment of peptic ulcer and ulcerative colitis. No side effects were reported on liver and kidney functions upon prolonged oral administration of this compounds. |
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Keywords: | Liver functions Ulcers Dexamesathone Quinazoline Acetamide Ulcerative colitis |
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