Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents

doi:10.1016/j.bmcl.2017.12.005

	Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents
	Ding, Shi 2,3; Dai, Rui-Yang 1; Wang, Wen-Ke 3; Cao, Qiao 3; Lan, Le-Fu3 ; Zhou, Xian-Li 1; Yang, Yu-She3
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2018-01-15
卷号	28 期号:2 页码:94-102
关键词	Gram-negative bacteria infection LpxC inhibitor Structure-activity relationship Zinc binding group Liver microsomal stability
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2017.12.005
文献子类	Article
英文摘要	LpxC inhibitors are new-type antibacterial agents developed in the last twenty years, mainly against Gram-negative bacteria infections. To develop novel LpxC inhibitors with good antibacterial activities and biological metabolism, we summarized the basic skeleton of reported LpxC inhibitors, designed and synthesized several series of compounds and tested their antibacterial activities against Escherichial coli and Pseudomonas aeruginosa in vitro. Structure-activity relationships have been discussed in this article. The metabolism stability of YDL-2, YDL-5, YDL-8, YDL-14, YDL-20- YDL-23 have been evaluated in liver microsomes, which indicated that the 2-amino isopropyl group may be a preferred structure than the 2-hydroxy ethyl group in the design of LpxC inhibitors. (C) 2017 Elsevier Ltd. All rights reserved.
资助项目	Key New Drug Creation and Manufacturing Program of China[2014ZX09507009-016] ; Youth Project of Education Department of Liaoning Province[LQN201709]
WOS关键词	ANTIBIOTIC-ACTIVITY ; BIOSYNTHESIS ; DEACETYLASE ; INFECTIONS ; PATHOGENS ; ENDOTOXIN
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000423658000007
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/272282]
专题	药物化学研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Zhou, Xian-Li; Yang, Yu-She
作者单位	1.Southwest Jiaotong Univ, Sch Life Sci & Engn, Chengdu 610031, Sichuan, Peoples R China 2.Liaoning Univ, Coll Pharm, Key Lab New Drug Res & Dev Liaoning Prov, Shenyang 10036, Liaoning, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Ding, Shi,Dai, Rui-Yang,Wang, Wen-Ke,et al. Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2018,28(2):94-102.
APA	Ding, Shi.,Dai, Rui-Yang.,Wang, Wen-Ke.,Cao, Qiao.,Lan, Le-Fu.,...&Yang, Yu-She.(2018).Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,28(2),94-102.
MLA	Ding, Shi,et al."Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 28.2(2018):94-102.