title: Synthesis, biological evaluation and molecular docking of quinazoline-4(1H)-one derivatives as anti-inflammatory and analgesic agents.
abstract: Two series of 2-phenyl-4(3H) quinazolinone derivatives have been synthesized. Most of the tested quinazolinone derivatives showed considerable potent anti-inflammatory and analgesic activity of superior GIT safety profile in experimental rats in comparing to indomethacin as reference drug. Compounds VIa, VIb were the most potent anti-inflammatory in experimental rats in comparing to indomethacin as reference drug. Docking study into COX-2 has been made for derivatives of anti-inflammatory activity.
authors.affiliation: Faculty of Pharmacy, Helwan University, Egypt.
authors.forename: Mosaad S
authors.initials: MS
authors.lastname: Mohamed
authors.forename: Mohsen M
authors.initials: MM
authors.lastname: Kamel
authors.forename: Emad M M
authors.initials: EM
authors.lastname: Kassem
authors.forename: Nageh
authors.initials: N
authors.lastname: Abotaleb
authors.forename: M
authors.initials: M
authors.lastname: Khedr
authors.forename: Marwa F
authors.initials: MF
authors.lastname: Ahmed
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002351:Carrageenan; D051546:Cyclooxygenase 2 / Q000737:chemistry / Q000378:metabolism; D015195:Drug Design; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D006358:Hot Temperature; D007213:Indomethacin / Q000737:chemistry; D008297:Male; D051379:Mice; D008958:Models, Molecular; D010147:Pain Measurement / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D011930:Reaction Time / Q000187:drug effects; D013276:Stomach Ulcer / Q000139:chemically induced; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D011799:Quinazolines; D002351:Carrageenan; D051546:Cyclooxygenase 2; D007213:Indomethacin