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  • Title: New 1,3,4-oxadiazole/oxime hybrids: Design, synthesis, anti-inflammatory, COX inhibitory activities and ulcerogenic liability.
    Author: Abd-Ellah HS, Abdel-Aziz M, Shoman ME, Beshr EAM, Kaoud T, Ahmed AFF.
    Journal: Bioorg Chem; 2017 Oct; 74():15-29. PubMed ID: 28738249.
    Abstract:
    A series of new 1,3,4-oxadiazole/oxime hybrids were synthesized and designed as potent COX inhibitors. The prepared compounds were evaluated for their anti-inflammatory, antioxidant and ulcerogenic activities. The results indicated that the prepared compounds exhibited remarkable anti-inflammatory activity with (69.60-109.60% of indomethacin activity) after 4h. In vitro COX inhibitory assay showed that compounds 6d and 7h are potent COX inhibitors with IC50 of (1.10-0.94) and (2.30-5.00) µM on both COX-1 and COX-2 respectively. Compound 7h was found to inhibit both COXs non-competitively with Ki values of 73µM and 89µM. Most of the tested compounds showed ulcer-free stomachs compared to indomethacin.
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