Design, synthesis and biological evaluation of LpxC inhibitors with novel hydrophilic terminus
文献类型：期刊论文
| 作者 | Ding, Shi1; Wang, Wen-Ke2; Cao, Qiao1; Chu, Wen-Jing1; Lan, Le-Fu1 ; Hu, Wen-Hao2; Yang, Yu-She1
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| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2015-06 |
| 卷号 | 26期号:6页码:763-767 |
| 关键词 | LpxC CHIR-090 Kojic acid derivatives Methylsulfone derivatives Metabolic stability |
| ISSN号 | 1001-8417 |
| DOI | 10.1016/j.cclet.2015.03.029 |
| 文献子类 | Article |
| 英文摘要 | In order to develop novel LpxC inhibitors with good activities and metabolic stability, two series of compounds with hydrophilic terminus have been synthesized and their in vitro antibacterial activities against Escherichial coli and Pseudomonas aeruginosa were evaluated. Especially, compounds 22b and c exhibited comparable antibacterial activities to CHIR-090 and better metabolic stability than CHIR-090 and LPC-011 in liver microsomes (rat and mouse), which indicated the terminal methylsulfone may be a preferred structure in the design of LpxC inhibitors and worthy of further investigations. (C) 2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved. |
| WOS关键词 | GRAM-NEGATIVE INFECTIONS ; ANTIBACTERIAL AGENTS ; ANTIBIOTIC-ACTIVITY ; DEACETYLASE LPXC ; BIOSYNTHESIS ; ENDOTOXIN |
| 资助项目 | National Science and Technology Major Project[00000000] ; Key New Drug Creation and Manufacturing Program, China[2014ZX09507009-016] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5464372 |
| WOS记录号 | WOS:000357224900029 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276504]  |
| 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 | Yang, Yu-She |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.E China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ding, Shi,Wang, Wen-Ke,Cao, Qiao,et al. Design, synthesis and biological evaluation of LpxC inhibitors with novel hydrophilic terminus[J]. CHINESE CHEMICAL LETTERS,2015,26(6):763-767. |
| APA | Ding, Shi.,Wang, Wen-Ke.,Cao, Qiao.,Chu, Wen-Jing.,Lan, Le-Fu.,...&Yang, Yu-She.(2015).Design, synthesis and biological evaluation of LpxC inhibitors with novel hydrophilic terminus.CHINESE CHEMICAL LETTERS,26(6),763-767. |
| MLA | Ding, Shi,et al."Design, synthesis and biological evaluation of LpxC inhibitors with novel hydrophilic terminus".CHINESE CHEMICAL LETTERS 26.6(2015):763-767. |
入库方式： OAI收割
来源：上海药物研究所
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