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  • Title: Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity.
    Author: Abouzid K, Bekhit SA.
    Journal: Bioorg Med Chem; 2008 May 15; 16(10):5547-56. PubMed ID: 18430576.
    Abstract:
    Herein, we report the design, synthesis, and pharmacological properties of a series of arylethenylpyridazinones 3a-h and arylethylpyridazinone derivatives 3k-i from the corresponding aryloxohexenoic 1a-e and aryloxohexanoic acids 2a,d, respectively. The synthesized compounds were tested for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Compound 3j demonstrated the greatest in vivo activity with ED(50) equal to 17mumol compared with celecoxib with no ulceration on the gastric mucosa. Docking study of the synthesized compounds into the active site of COX-2 revealed a similar binding mode to RS-57067, a COX-2 inhibitor.
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