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1.
J Enzyme Inhib Med Chem ; 23(2): 225-9, 2008 Apr.
Article in English | MEDLINE | ID: mdl-18343908

ABSTRACT

Antioxidants are compounds that can delay, inhibit, or prevent the oxidation of materials that can be oxidized by scavenging free radicals and help in diminishing oxidative stress. They belong to different chemical classes. Recently there are studies related to pyridazinone derivatives for their antioxidant activities. Since there are evidences implicates reactive oxygen species and nitric oxide as mediators of inflammation and/or tissue damage in inflammatory and arthritic disorders it was though that compounds that have both antioxidant and anti-inflammatory activities would have been essential for the inflammatory diseases. Based on these findings a series of 2H-pyridazine-3-one and 6-chloropyridazine analogues that have anti-inflammatory activity was tested in vitro on superoxide formation and effects on lipid peroxidation were determined against alpha-tocopherol. Most of the compounds have strong inhibitory effect on superoxide anion (between 84% - 99%) at 10(- 3) M concentration. In addition, these compounds showed similar activity to alpha-tocopherol at 10(- 3) M concentrations.


Subject(s)
Antioxidants/chemistry , Antioxidants/pharmacology , Pyridazines/chemistry , Pyridazines/pharmacology , Chlorine Compounds/chemistry , Chlorine Compounds/pharmacology , Drug Evaluation, Preclinical , Lipid Peroxidation/drug effects , Molecular Structure , Structure-Activity Relationship , Superoxides/chemistry
2.
Arch Pharm Res ; 28(5): 509-17, 2005 May.
Article in English | MEDLINE | ID: mdl-15974435

ABSTRACT

A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4-chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analgesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.


Subject(s)
Analgesics/chemical synthesis , Anti-Inflammatory Agents/chemical synthesis , Acetamides/chemical synthesis , Acetamides/pharmacology , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Mice , Pyrazoles/chemical synthesis , Pyrazoles/pharmacology , Pyridazines/chemical synthesis , Pyridazines/pharmacology
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