title: Synthesis of some new 2-(substituted-phenyl)-5-(N,N-diphenylaminomethyl)-1,3,4-oxadiazoles: a safer anti-inflammatory and analgesic agents.
abstract: A series of 2-(substituted-phenyl)-5-(N,N-diphenylaminomethyl)-1,3,4-oxadiazoles (3-15) were synthesized. The compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation actions. The percentage inhibition in edema at different time intervals indicated that compounds 8, 11, 12, 14 and 15 exhibited good anti-inflammatory potential. The results illustrate that 2-(2-acetoxyphenyl)-5-(N,N-diphenylaminomethyl)-1,3,4-oxadiazole (15) and 2-(3,4-dimethoxyphenyl)-5-(N,N-diphenylaminomethyl)-1,3,4-oxadiazole (12) showed best anti-inflammatory activity among the series tested. Furthermore, activity is higher in case of chloro substitution as compared to methyl substitution. The compounds synthesized were also evaluated for their ulcerogenic and lipid peroxidation action and showed superior GI safety profile along with reduction in lipid peroxidation as compared to that of ibuprofen.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, New Delhi-110062, India.
authors.forename: Aditya Kumar
authors.initials: AK
authors.lastname: Kataria
authors.forename: Suroor Ahmad
authors.initials: SA
authors.lastname: Khan
authors.forename: Mohammad Mumtaz
authors.initials: MM
authors.lastname: Alam
authors.forename: Asif
authors.initials: A
authors.lastname: Husain
authors.forename: Mymoona
authors.initials: M
authors.lastname: Akhtar
authors.forename: Suruchi
authors.initials: S
authors.lastname: Khanna
authors.forename: Rashiduddin
authors.initials: R
authors.lastname: Haider
authors.forename: Rashid
authors.initials: R
authors.lastname: Haider
authors.forename: Mohammad
authors.initials: M
authors.lastname: Shaquiquzzaman
mesh_terms: D019342:Acetic Acid; D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002351:Carrageenan; D004195:Disease Models, Animal; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control; D015227:Lipid Peroxidation / Q000187:drug effects; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D010146:Pain / Q000139:chemically induced / Q000517:prevention & control; D010147:Pain Measurement; D010437:Peptic Ulcer / Q000139:chemically induced; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D010069:Oxadiazoles; D002351:Carrageenan; D019342:Acetic Acid