Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents
文献类型：期刊论文
| 作者 | Ding, Shi2,3; Dai, Rui-Yang1; Wang, Wen-Ke3; Cao, Qiao3; Lan, Le-Fu3 ; Zhou, Xian-Li1; Yang, Yu-She3
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 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. |
| WOS关键词 | ANTIBIOTIC-ACTIVITY ; BIOSYNTHESIS ; DEACETYLASE ; INFECTIONS ; PATHOGENS ; ENDOTOXIN |
| 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研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000423658000007 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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