Synthesis and biological evaluation of Aspergillomarasmine A derivatives   as novel NDM-1 inhibitor to overcome antibiotics resistance

doi:10.1016/j.bmc.2017.07.025

CORC > 北京大学 > 化学与分子工程学院

	Synthesis and biological evaluation of Aspergillomarasmine A derivatives as novel NDM-1 inhibitor to overcome antibiotics resistance
	Zhang, Jian ; Wang, Sanshan ; Wei, Qi ; Guo, Qianqian ; Bai, Yingjie ; Yang, Shaoqiang ; Song, Fuhang ; Zhang, Lixin ; Lei, Xiaoguang
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2017
关键词	Aspergillomarasmine A Antibiotic resistance Metallo-beta-lactamases NDM-1 Antibiotics BETA-LACTAMASE INHIBITORS BACTERIA
DOI	10.1016/j.bmc.2017.07.025
英文摘要	The beta-lactam antibiotic resistance of Gram-negative bacteria has shown to be a critical global health problem. One of the primary reasons for the drug resistance is the existence of beta-lactamases especially metallo-beta-lactamases such as New Delhi metallo-beta-lactamase (NDM-1) and Verona Integron-encoded metallo-beta-lactamase (VIM-2). The fungal natural product Aspergillomarasmine A (AMA) has proven to be a promising inhibitor of NDM-1 and VIM-2 both in vitro and in vivo. Seven new analogues of AMA were synthesized by utilizing different strategies. The biological evaluation of these analogues was performed to study the structure-activity relationship of AMA both in vitro and in vivo. Remarkably, the lead compound 4 showed synergistic effect in combination with Meropenem to overcome the antibiotic resistance of the Gram-negative bacteria such as K. pneumoniae (BAA-2146) expressing NDM-1. (C) 2017 Elsevier Ltd. All rights reserved.; National High Technology Project 973 [2015CB856200]; NNSFC [21472010, 21521003, 21561142002, 21625201]; SCI(E); ARTICLE; 19,SI; 5133-5141; 25
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/484779]
专题	化学与分子工程学院生命科学学院
推荐引用方式 GB/T 7714	Zhang, Jian,Wang, Sanshan,Wei, Qi,et al. Synthesis and biological evaluation of Aspergillomarasmine A derivatives as novel NDM-1 inhibitor to overcome antibiotics resistance[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2017.
APA	Zhang, Jian.,Wang, Sanshan.,Wei, Qi.,Guo, Qianqian.,Bai, Yingjie.,...&Lei, Xiaoguang.(2017).Synthesis and biological evaluation of Aspergillomarasmine A derivatives as novel NDM-1 inhibitor to overcome antibiotics resistance.BIOORGANIC & MEDICINAL CHEMISTRY.
MLA	Zhang, Jian,et al."Synthesis and biological evaluation of Aspergillomarasmine A derivatives as novel NDM-1 inhibitor to overcome antibiotics resistance".BIOORGANIC & MEDICINAL CHEMISTRY (2017).