Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity
Abouzid, Khaled; Bekhit, Salma A;
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.
Other data
| Title | Novel anti-inflammatory agents based on pyridazinone scaffold; design, synthesis and in vivo activity | Authors | Abouzid, Khaled ; Bekhit, Salma A | Keywords | pyridazinone;anti-inflammatory;selective COX-2 inhibitors;docking study;SELECTIVE CYCLOOXYGENASE-2 INHIBITORS;BIOLOGICAL EVALUATION;COX-2 INHIBITORS;POTENT;IDENTIFICATION;DERIVATIVES;MECHANISM | Issue Date | 15-May-2008 | Publisher | PERGAMON-ELSEVIER SCIENCE LTD | Journal | Bioorganic & medicinal chemistry | Volume | 16 | Issue | 10 | Start page | 5547 | End page | 5556 | ISSN | 0968-0896 | DOI | 10.1016/j.bmc.2008.04.007 | PubMed ID | 18430576 | Scopus ID | 2-s2.0-43749101130 | Web of science ID | WOS:000256052400019 |
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