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: | , , , , |
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| Format: | Article |
| Language: | English English English |
| Published: |
Elsevier
2018
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| Subjects: | |
| Online Access: | 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 http://irep.iium.edu.my/63145/ https://ac.els-cdn.com/S1319016417301676/1-s2.0-S1319016417301676-main.pdf?_tid=8c31153c-8e3d-4c0f-922b-c96299d9e215&acdnat=1522114348_d2a12a36aa8688eedf102b32855f6f72 |
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| Institution: | Universiti Islam Antarabangsa Malaysia |
| Language: | English English English |
| Summary: | 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. |
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