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New pentadienone oxime ester derivatives: synthesis and anti-inflammatory activity.

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-?B 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.

SUBMITTER: Li Q

PROVIDER: S-EPMC6010105 | biostudies-other | 2018 Dec

REPOSITORIES: biostudies-other

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New pentadienone oxime ester derivatives: synthesis and anti-inflammatory activity.

Li Qin Q Zhang Juping J Chen Liu Zeng LZ Wang Jie Quan JQ Zhou Hai Ping HP Tang Wen Jian WJ Xue Wei W Liu Xin Hua XH

Journal of enzyme inhibition and medicinal chemistry 20181201 1

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 value ...[more]

PMID: 29199491

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