Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity
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-aminosulphonyl...
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| Format: | Article |
| Language: | English |
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Elsevier
2018-01-01
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| Series: | Saudi Pharmaceutical Journal |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016417301676 |
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| author | Fatmah A.S. Alasmary Amani S. Awaad Ahmed M. Alafeefy Reham M. El-Meligy Saleh I. Alqasoumi |
| author_facet | Fatmah A.S. Alasmary Amani S. Awaad Ahmed M. Alafeefy Reham M. El-Meligy Saleh I. Alqasoumi |
| author_sort | Fatmah A.S. Alasmary |
| collection | DOAJ |
| description | 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. Keywords: Liver functions, Ulcers, Dexamesathone, Quinazoline, Acetamide, Ulcerative colitis |
| first_indexed | 2024-12-22T22:04:57Z |
| format | Article |
| id | doaj.art-aafb917dd5fd413d9516033ad565f6aa |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-12-22T22:04:57Z |
| publishDate | 2018-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-aafb917dd5fd413d9516033ad565f6aa2022-12-21T18:11:00ZengElsevierSaudi Pharmaceutical Journal1319-01642018-01-01261138143Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activityFatmah A.S. Alasmary0Amani S. Awaad1Ahmed M. Alafeefy2Reham M. El-Meligy3Saleh I. Alqasoumi4Chemistry Department, College of Science, King Saud University, Riyadh 11362, Saudi ArabiaPharmacognosy Department, College of Pharmacy, Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia; Corresponding author at: Pharmacognosy Department, College of Pharmacy, Prince Sattam bin Abdulaziz University, P.O. Box 173, Al-Kharj, Riyadh 11942, Saudi Arabia.Department of Chemistry, Kulliyyah of Science, International Islamic University Malaysia, MalaysiaAromatic and Medicinal Plants Department, Desert Research Center, Cairo, EgyptDepartment of Pharmacognosy, College of Pharmacy, King Saud University, KSATwo 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. Keywords: Liver functions, Ulcers, Dexamesathone, Quinazoline, Acetamide, Ulcerative colitishttp://www.sciencedirect.com/science/article/pii/S1319016417301676 |
| spellingShingle | Fatmah A.S. Alasmary Amani S. Awaad Ahmed M. Alafeefy Reham M. El-Meligy Saleh I. Alqasoumi Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity Saudi Pharmaceutical Journal |
| title | Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity |
| title_full | Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity |
| title_fullStr | Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity |
| title_full_unstemmed | Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity |
| title_short | Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity |
| title_sort | novel quinazoline and acetamide derivatives as safe anti ulcerogenic agent and anti ulcerative colitis activity |
| url | http://www.sciencedirect.com/science/article/pii/S1319016417301676 |
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