title: Synthesis and biological evaluation of certain 3-substituted benzylideneamino-2-(4-nitrophenyl)quinazolin-4(3H)-one derivatives.
abstract: Certain new 3H-quinazolin-4-one Schiff's bases were synthesized and screened for their activities against ulcerative colitis "UC". Their activity against phospholipase A2 and protease enzymes was also investigated. Some compounds possessed remarkable effect with different potentials against acetic acid-induced colitis model in rats. Compound 14 (50 mg/kg) was more effective than dexamesathone (0.01 mg/kg). It produced 79.78% protection of control colitis; however, compound 13 produced 75.80% protection and was considered as effective as dexamesathone with 75.30% protection. The observed results could be explained partially by their anti-inflammatory activities which appear as phospholipase A2 (hGIIA) and/or through protease inhibitor potentials. However, all the compounds under test showed preferential inhibition towards hG-IIA type of PLA2 rather than DrG-IB with varying degrees. Interestingly, compounds 14, 13, 12 and 11 displayed excellent inhibitory activity against phospholipase A2 accompanied by protease inhibitory profile.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, Salman bin Abdulaziz University , Al-Kharj , Saudi Arabia .
authors.forename: Ahmed M
authors.initials: AM
authors.lastname: Alafeefy
authors.forename: Amani S
authors.initials: AS
authors.lastname: Awaad
authors.forename: Hatem A
authors.initials: HA
authors.lastname: Abdel-Aziz
authors.forename: Reham M
authors.initials: RM
authors.lastname: El-Meligy
authors.forename: Mohamed E
authors.initials: ME
authors.lastname: Zain
authors.forename: Mounerah R
authors.initials: MR
authors.lastname: Al-Outhman
authors.forename: Abir B
authors.initials: AB
authors.lastname: Bacha
mesh_terms: D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D001597:Benzylidene Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D003093:Colitis, Ulcerative / Q000188:drug therapy* / Q000517:prevention & control; D004195:Disease Models, Animal; D015195:Drug Design; D005260:Female; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010447:Peptide Hydrolases / Q000378:metabolism; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D017208:Rats, Wistar
chemical_list: D000897:Anti-Ulcer Agents; D001597:Benzylidene Compounds; D052999:Quinazolinones; D010447:Peptide Hydrolases
keywords: Phospholipase A2; protease; quinazoline; schiff’s bases; ulcerative colitis