title: Synthesis of novel 1,3,4-trisubstituted pyrazoles as anti-inflammatory and analgesic agents.
abstract: Some novel 1,3,4-trisubstituted pyrazoles were synthesized and screened for their anti-inflammatory and analgesic activities as well as their ulcerogenic liability. They showed anti-inflammatory and analgesic activities with better GIT tolerance than the standard drug phenylbutazone. In addition, IC50 values for 5e and 8e were recorded. Compound 5e was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, COX-1/COX-2 isozyme selectivity was also done which showed equal inhibition to both isoforms.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, P.O. Box 11562, Cairo, Egypt.
authors.forename: Fatma A
authors.initials: FA
authors.lastname: Ragab
authors.forename: Nagwa M
authors.initials: NM
authors.lastname: Abdel Gawad
authors.forename: Hanan H
authors.initials: HH
authors.lastname: Georgey
authors.forename: Mona F
authors.initials: MF
authors.lastname: Said
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016227:Benzoquinones; D002351:Carrageenan; D051545:Cyclooxygenase 1 / Q000378:metabolism; D051546:Cyclooxygenase 2 / Q000378:metabolism; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D008297:Male; D051379:Mice; D008956:Models, Chemical; D015394:Molecular Structure; D010146:Pain / Q000139:chemically induced / Q000517:prevention & control; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D016227:Benzoquinones; D016861:Cyclooxygenase Inhibitors; D011720:Pyrazoles; C004532:quinone; D002351:Carrageenan; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human