designsynthesisandbiologicalevaluationoflpxcinhibitorswithnovelhydrophilicterminus
文献类型：期刊论文
| 作者 | Ding Shi1; Wang Wenke2; Cao Qiao1; Chu Wenjing1; Lan Lefu1 ; Hu Wenhao2; Yang Yushe1
|
| 刊名 | chinesechemicalletters
 |
| 出版日期 | 2015 |
| 卷号 | 26期号:6页码:763 |
| 关键词 | GRAM-NEGATIVE INFECTIONS ANTIBACTERIAL AGENTS ANTIBIOTIC-ACTIVITY DEACETYLASE LPXC BIOSYNTHESIS ENDOTOXIN LpxC CHIR-090 Kojic acid derivatives Methylsulfone derivatives Metabolic stability |
| ISSN号 | 1001-8417 |
| DOI | 10.1016/j.cclet.2015.03.029 |
| 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. |
| 资助项目 | [National Science and Technology Major Project] ; [Key New Drug Creation and Manufacturing Program, China] |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/285900]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国科学院上海药物研究所 2.华东师范大学 |
| 推荐引用方式 GB/T 7714 | Ding Shi,Wang Wenke,Cao Qiao,et al. designsynthesisandbiologicalevaluationoflpxcinhibitorswithnovelhydrophilicterminus[J]. chinesechemicalletters,2015,26(6):763. |
| APA | Ding Shi.,Wang Wenke.,Cao Qiao.,Chu Wenjing.,Lan Lefu.,...&Yang Yushe.(2015).designsynthesisandbiologicalevaluationoflpxcinhibitorswithnovelhydrophilicterminus.chinesechemicalletters,26(6),763. |
| MLA | Ding Shi,et al."designsynthesisandbiologicalevaluationoflpxcinhibitorswithnovelhydrophilicterminus".chinesechemicalletters 26.6(2015):763. |
入库方式： OAI收割
来源：上海药物研究所
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