Design, synthesis and biological evaluation of C(4) substituted monobactams as antibacterial agents against multidrug-resistant Gram-negative bacteria
文献类型：期刊论文
| 作者 | Kou, Qunhuan1,2; Wang, Ting3; Zou, Feng3; Zhang, Shuhua3; Chen, Qian1,2; Yang, Yushe1,2
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2018-05-10 |
| 卷号 | 151页码:98-109 |
| ISSN号 | 0223-5234 |
| 关键词 | Monobactam C(4) substituents Pyridone MDR Gram-negative bacteria Antibacterial activity |
| DOI | 10.1016/j.ejmech.2018.03.058 |
| 文献子类 | Article |
| 英文摘要 | A series of novel pyridone conjugated monobactams with various substituents at the (4) position were synthesized and evaluated for their antibacterial activities against a panel of multidrug-resistant (MDR) Gram-negative bacteria in vitro. Compounds 46d, 54 and 75e displayed good to moderate activities against P. aeruginosa, among which the activity of 75e against P. aeruginosa was comparable to that of BAL30072 under iron limitation condition. Compounds 35, 46d, 54, 56a, 56c and 56d exhibited good to excellent antibacterial activities against E. coli and K. pneumoniae, which were comparable or superior to that of BAL30072. In vitro liver microsomal stability was further evaluated and the results manifested that Compounds 35, 46d and 54 were metabolically stable in human liver microsomes. (C) 2018 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | BETA-LACTAM ANTIBIOTICS ; PSEUDOMONAS-AERUGINOSA ; AMINOTHIAZOLYLGLYCYL DERIVATIVES ; ACINETOBACTER-BAUMANNII ; DRUG DISCOVERY ; CEPHALOSPORIN ; ACID ; PHARMACOKINETICS ; INFECTIONS ; MECHANISMS |
| 资助项目 | National Natural Science Foundation of China[81573284] ; National Science and Technology Major Project of China[2014ZX09507009-013] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| WOS记录号 | WOS:000432640900008 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279761]  |
| 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, Yushe |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Sichuan Primed Shines Biotech Co Ltd, Dept Microbiol, Chengdu 610041, Sichuan, Peoples R China |
| 推荐引用方式 GB/T 7714 | Kou, Qunhuan,Wang, Ting,Zou, Feng,et al. Design, synthesis and biological evaluation of C(4) substituted monobactams as antibacterial agents against multidrug-resistant Gram-negative bacteria[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,151:98-109. |
| APA | Kou, Qunhuan,Wang, Ting,Zou, Feng,Zhang, Shuhua,Chen, Qian,&Yang, Yushe.(2018).Design, synthesis and biological evaluation of C(4) substituted monobactams as antibacterial agents against multidrug-resistant Gram-negative bacteria.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,151,98-109. |
| MLA | Kou, Qunhuan,et al."Design, synthesis and biological evaluation of C(4) substituted monobactams as antibacterial agents against multidrug-resistant Gram-negative bacteria".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 151(2018):98-109. |
入库方式： OAI收割
来源：上海药物研究所
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