| Objective:Many natural products that appear in the natural product have a basic core skeleton that contains a?-lactone ring.Compounds containing a?-butyrolactone ring generally exhibit a wide variety of biological activities.The purpose of this study was to design and synthesize compounds with multiple core skeletons as?-lactone rings and detect their anti-inflammatory activity.Methods:Based on previous laboratory studies on halogenated lactones,this study designed 24 deactivated olefins 2a2x??,?-unsaturated enones?,through the halogenation of 2a2x,a total of 28 novel?-butyrolactone derivatives were obtained.The anti-inflammatory activity of?-butyrolactone derivatives was detected by reducing ROS and NO levels in RAW 264.7 cells.Results:1.24 novel deactivated olefins 2a2x??,?-unsaturated enones?and 28 novel?-butyrolactone derivatives were synthesized.A total of 62 new compounds were synthesized and the structures were all subjected to 1H-NMR and 13C-NMR structures.It was confirmed that deactivated olefins??,?-unsaturated enones?can also be brominated to give?-lactone rings and the yield is extremely high.2.Activity test results:?1?The target compounds 3h can significantly reduce ROS levels in RAW 264.7cells;?2?The target compound 3h and 3y can significantly reduce the NO level in RAW 264.7 cells.Only the dose of 3y-1 reaches 20mM,the NO level in RAW 264.7cells can be decreased,and ent-3h had no significant effect on the two assays.ConclusionExperiments have shown the compounds of the?-butyrolactone ring structure are novel,simple synthesis method,high yield,and good anti-inflammatory activity.It has also been demonstrated that inactive olefins??,?-unsaturated enones?can also be halogenated lactones into rings.And compounds 3h can be used as potentially potent anti-inflammatory agents.The structure of 24 novel?,?-unsaturated enones and 28novel?-butyrolactone derivatives was confirmed by 1H-NMR,13C-NMR and HRMS. |
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