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-tolyl3H-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- aminosulpho...

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Main Authors: Alasmary, Fatmah A.S., Awaad, Amani Shafeek, Alafeefy, Ahmed Mahmoud, El-Meligy, Reham M., Alqasoumi, Saleh Ibrahim
Format: Article
Language:English
English
English
Published: Elsevier 2018
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Online Access:http://irep.iium.edu.my/63145/
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http://irep.iium.edu.my/63145/
http://irep.iium.edu.my/63145/1/63145-%20Novel%20quinazoline%20and%20acetamide%20derivatives%20as%20safe%20anti-ulcerogenic.pdf
http://irep.iium.edu.my/63145/19/55862%20Novel%20quinazoline%20and%20acetamide%20SCOPUS.pdf
http://irep.iium.edu.my/63145/13/63145_Novel%20quinazoline%20and%20acetamide%20derivatives_wos.pdf
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spelling iium-631452019-01-30T00:49:47Z http://irep.iium.edu.my/63145/ Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity Alasmary, Fatmah A.S. Awaad, Amani Shafeek Alafeefy, Ahmed Mahmoud El-Meligy, Reham M. Alqasoumi, Saleh Ibrahim T Technology (General) Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl3H-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 & AntiUlcerative 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. Elsevier 2018 Article PeerReviewed application/pdf en http://irep.iium.edu.my/63145/1/63145-%20Novel%20quinazoline%20and%20acetamide%20derivatives%20as%20safe%20anti-ulcerogenic.pdf application/pdf en http://irep.iium.edu.my/63145/19/55862%20Novel%20quinazoline%20and%20acetamide%20SCOPUS.pdf application/pdf en http://irep.iium.edu.my/63145/13/63145_Novel%20quinazoline%20and%20acetamide%20derivatives_wos.pdf Alasmary, Fatmah A.S. and Awaad, Amani Shafeek and Alafeefy, Ahmed Mahmoud and El-Meligy, Reham M. and Alqasoumi, Saleh Ibrahim (2018) Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity. Saudi Pharmaceutical Journal, 26 (1). pp. 138-143. ISSN 1319-0164 https://ac.els-cdn.com/S1319016417301676/1-s2.0-S1319016417301676-main.pdf?_tid=8c31153c-8e3d-4c0f-922b-c96299d9e215&acdnat=1522114348_d2a12a36aa8688eedf102b32855f6f72 10.1016/j.jsps.2017.09.011
repository_type Digital Repository
institution_category Local University
institution International Islamic University Malaysia
building IIUM Repository
collection Online Access
language English
English
English
topic T Technology (General)
spellingShingle T Technology (General)
Alasmary, Fatmah A.S.
Awaad, Amani Shafeek
Alafeefy, Ahmed Mahmoud
El-Meligy, Reham M.
Alqasoumi, Saleh Ibrahim
Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity
description Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl3H-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 & AntiUlcerative 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.
format Article
author Alasmary, Fatmah A.S.
Awaad, Amani Shafeek
Alafeefy, Ahmed Mahmoud
El-Meligy, Reham M.
Alqasoumi, Saleh Ibrahim
author_facet Alasmary, Fatmah A.S.
Awaad, Amani Shafeek
Alafeefy, Ahmed Mahmoud
El-Meligy, Reham M.
Alqasoumi, Saleh Ibrahim
author_sort Alasmary, Fatmah A.S.
title 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_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_sort novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity
publisher Elsevier
publishDate 2018
url http://irep.iium.edu.my/63145/
http://irep.iium.edu.my/63145/
http://irep.iium.edu.my/63145/
http://irep.iium.edu.my/63145/1/63145-%20Novel%20quinazoline%20and%20acetamide%20derivatives%20as%20safe%20anti-ulcerogenic.pdf
http://irep.iium.edu.my/63145/19/55862%20Novel%20quinazoline%20and%20acetamide%20SCOPUS.pdf
http://irep.iium.edu.my/63145/13/63145_Novel%20quinazoline%20and%20acetamide%20derivatives_wos.pdf
first_indexed 2023-09-18T21:29:36Z
last_indexed 2023-09-18T21:29:36Z
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