title: Synthesis and biological evaluation of some new pyridazinone derivatives.
abstract: A series of pyridazinone derivatives (19-34) were synthesized with an aim to synthesize safer anti-inflammatory agents. The compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation (LPO) actions. The percentage inhibition in edema at different time intervals indicated that compounds 20, 26, 28 and 34 exhibited good anti-inflammatory potential, comparable with that of ibuprofen (85.77%) within a range of 67.48-77.23%. The results illustrate that 5-(4-fluoro-benzyl)-3-(4-chloro-phenyl)-1,6-dihydro-6-pyridazinone (26) and 5-(4-chloro-benzyl)-3-(4-chloro-phenyl)-1,6-dihydro-6-pyridazinone (20) showed best anti-inflammatory activity. Furthermore, activity is more in case of chloro substitution as compared with methyl-substitution. The compounds synthesized were also evaluated for their ulcerogenic and LPO action and showed superior gastrointestinal safety profile along with reduction in LPO as compared with that of the ibuprofen.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi, India. drasifhusain@yahoo.com
authors.forename: Asif
authors.initials: A
authors.lastname: Husain
authors.forename: Sushma
authors.initials: S
authors.lastname: Drabu
authors.forename: Nitin
authors.initials: N
authors.lastname: Kumar
authors.forename: M Mumtaz
authors.initials: MM
authors.lastname: Alam
authors.forename: Aftab
authors.initials: A
authors.lastname: Ahmad
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007052:Ibuprofen / Q000494:pharmacology; D015227:Lipid Peroxidation / Q000187:drug effects; D015394:Molecular Structure; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D011724:Pyridazines; D007052:Ibuprofen