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  • Title: New pentadienone oxime ester derivatives: synthesis and anti-inflammatory activity.
    Author: Li Q, Zhang J, Chen LZ, Wang JQ, Zhou HP, Tang WJ, Xue W, Liu XH.
    Journal: J Enzyme Inhib Med Chem; 2018 Dec; 33(1):130-138. PubMed ID: 29199491.
    Abstract:
    To develop novel anti-inflammatory agents, a series of new pentadienone oxime ester compounds were designed and synthesized. The structures were determined by IR, 1H NMR, 13 C NMR, and HRMS. All compounds have been screened for their anti-inflammatory activity by evaluating their inhibition against LPS-induced nitric oxide (NO) release in RAW 264.7 cell. Among them, compound 5j was found to be one of the most potent compounds in inhibiting NO and IL-6 (IC50 values were 6.66 µM and 5.07 µM, respectively). Preliminary mechanism studies show that title compound 5j could significantly suppress expressions of nitric oxide synthase, COX-2, and NO, IL-6 through Toll-like receptor 4/mitogen-activated protein kinases/NF-κB signalling pathway. These data support further studies to assess rational design of more efficient pentadienone oxime ester derivatives with anti-inflammatory activity in the future.
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