胡椒碱类似物作为有效的金黄色葡萄球菌NorA外排泵抑制剂。
Piperine analogs as potent Staphylococcus aureus NorA efflux pump inhibitors.
作者信息
Sangwan Payare L, Koul Jawahir L, Koul Surrinder, Reddy Mallepally V, Thota Niranjan, Khan Inshad A, Kumar Ashwani, Kalia Nitin P, Qazi Ghulam N
机构信息
Bioorganic Chemistry Division, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu Tawi 180001, India.
出版信息
Bioorg Med Chem. 2008 Nov 15;16(22):9847-57. doi: 10.1016/j.bmc.2008.09.042. Epub 2008 Sep 19.
Based on our recent findings that piperine is a potent Staphylococcus aureus NorA efflux pump inhibitor (EPI), 38 piperine analogs were synthesized and bioevaluated for their EPI activity. Twenty-five of them were found active with potentiating activity equivalent or more than known EPIs like reserpine, carsonic acid and verapamil. The inhibitory mechanism of the compounds was confirmed by efflux inhibition assay using ethidium bromide as NorA substrate. The present communication describes the synthesis, bioevaluation and structure related activity of these efflux pump inhibitors.
基于我们最近的发现，即胡椒碱是一种有效的金黄色葡萄球菌NorA外排泵抑制剂（EPI），合成了38种胡椒碱类似物，并对其EPI活性进行了生物评价。发现其中25种具有活性，其增强活性与利血平、卡索尼酸和维拉帕米等已知EPI相当或更高。使用溴化乙锭作为NorA底物的外排抑制试验证实了这些化合物的抑制机制。本通讯描述了这些外排泵抑制剂的合成、生物评价及结构相关活性。
Zotero 插件