• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

基于磺胺的非炔类LpxC抑制剂作为革兰氏阴性抗菌剂。

Sulfonamide-based non-alkyne LpxC inhibitors as Gram-negative antibacterial agents.

作者信息

Kawai Tetsuya, Kazuhiko Iwase, Takaya Noriko, Yamaguchi Yuko, Kishii Ryuta, Kohno Yasushi, Kurasaki Haruaki

机构信息

Watarase Research Center, Kyorin Pharmaceutical Co., Ltd., 1848 Nogi, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan.

Watarase Research Center, Kyorin Pharmaceutical Co., Ltd., 1848 Nogi, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan.

出版信息

Bioorg Med Chem Lett. 2017 Feb 15;27(4):1045-1049. doi: 10.1016/j.bmcl.2016.12.059. Epub 2016 Dec 24.

DOI:10.1016/j.bmcl.2016.12.059
PMID:28082037
Abstract

We attempted to optimize sulfonamide-based non-alkyne LpxC inhibitors by focusing on improvements in enzyme inhibitory and antibacterial activity. It was discovered that inhibitors possessing 2-aryl benzofuran as a hydrophobe exhibited good activity. In particular, compound 21 displayed impressive antibacterial activity (E. coli MIC=0.063μg/mL, K. pneumoniae MIC=0.5μg/mL, and P. aeruginosa MIC=0.5μg/mL), and is a promising lead for further exploration as an antibacterial agent.

摘要

我们试图通过专注于提高酶抑制活性和抗菌活性来优化基于磺酰胺的非炔烃类LpxC抑制剂。结果发现，具有2-芳基苯并呋喃作为疏水基团的抑制剂表现出良好的活性。特别是化合物21表现出令人印象深刻的抗菌活性（大肠杆菌的最低抑菌浓度为0.063μg/mL，肺炎克雷伯菌的最低抑菌浓度为0.5μg/mL，铜绿假单胞菌的最低抑菌浓度为0.5μg/mL），是作为抗菌剂进一步探索的有前途的先导化合物。

相似文献

1
Sulfonamide-based non-alkyne LpxC inhibitors as Gram-negative antibacterial agents.基于磺胺的非炔类LpxC抑制剂作为革兰氏阴性抗菌剂。
Bioorg Med Chem Lett. 2017 Feb 15;27(4):1045-1049. doi: 10.1016/j.bmcl.2016.12.059. Epub 2016 Dec 24.
2
Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents.杂环甲基砜羟肟酸 LpxC 抑制剂作为革兰氏阴性抗菌剂。
Bioorg Med Chem Lett. 2012 Nov 15;22(22):6832-8. doi: 10.1016/j.bmcl.2012.09.058. Epub 2012 Sep 24.
3
Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents.新型LpxC抑制剂作为革兰氏阴性抗菌剂的设计、合成及构效关系评估
Bioorg Med Chem Lett. 2018 Jan 15;28(2):94-102. doi: 10.1016/j.bmcl.2017.12.005. Epub 2017 Dec 5.
4
Structure-based discovery of LpxC inhibitors.基于结构的LpxC抑制剂发现
Bioorg Med Chem Lett. 2017 Apr 15;27(8):1670-1680. doi: 10.1016/j.bmcl.2017.03.006. Epub 2017 Mar 6.
5
Recent Process in the Inhibitors of UDP-3-O-(R-3-hydroxyacyl)-Nacetylglucosamine Deacetylase (LpxC) Against Gram-Negative Bacteria.UDP-3-O-(R-3-羟酰基)-N-乙酰葡糖胺脱乙酰酶（LpxC）抑制剂抗革兰氏阴性菌的研究进展
Mini Rev Med Chem. 2018;18(4):310-323. doi: 10.2174/1389557516666161013120253.
6
High susceptibility of MDR and XDR Gram-negative pathogens to biphenyl-diacetylene-based difluoromethyl-allo-threonyl-hydroxamate LpxC inhibitors.耐多药和广泛耐药革兰氏阴性病原体对联苯二乙炔基二氟甲基-别苏氨酰异羟肟酸酯LpxC抑制剂高度敏感。
J Antimicrob Chemother. 2016 Oct;71(10):2874-82. doi: 10.1093/jac/dkw210. Epub 2016 Jun 20.
7
Antibacterial activities and characterization of novel inhibitors of LpxC.新型LpxC抑制剂的抗菌活性及特性
Antimicrob Agents Chemother. 2002 Jun;46(6):1793-9. doi: 10.1128/AAC.46.6.1793-1799.2002.
8
Synthesis and antimicrobial activity of novel benzoxazine sulfonamide derivatives.新型苯并恶嗪磺酰胺衍生物的合成及其抗菌活性
Bioorg Med Chem Lett. 2015 Apr 1;25(7):1643-6. doi: 10.1016/j.bmcl.2015.01.026. Epub 2015 Jan 20.
9
LpxC inhibitors: a patent review (2010-2016).LpxC抑制剂：专利综述（2010 - 2016年）
Expert Opin Ther Pat. 2017 Nov;27(11):1227-1250. doi: 10.1080/13543776.2017.1360282. Epub 2017 Aug 4.
10
High-throughput catch-and-release synthesis of oxazoline hydroxamates. Structure-activity relationships in novel inhibitors of Escherichia coli LpxC: in vitro enzyme inhibition and antibacterial properties.恶唑啉异羟肟酸酯的高通量捕获与释放合成。大肠杆菌LpxC新型抑制剂的构效关系：体外酶抑制和抗菌特性。
J Am Chem Soc. 2003 Feb 12;125(6):1575-86. doi: 10.1021/ja0209114.

引用本文的文献

1
Recent advances in small molecule LpxC inhibitors against gram-negative bacteria (2014-2024).2014 - 2024年针对革兰氏阴性菌的小分子LpxC抑制剂的最新进展
Front Microbiol. 2025 Feb 10;16:1541379. doi: 10.3389/fmicb.2025.1541379. eCollection 2025.
2
Development of Fragment-Based Inhibitors of the Bacterial Deacetylase LpxC with Low Nanomolar Activity.基于片段的细菌去乙酰化酶 LpxC 抑制剂的开发，具有低纳摩尔活性。
J Med Chem. 2024 Oct 10;67(19):17363-17391. doi: 10.1021/acs.jmedchem.4c01262. Epub 2024 Sep 20.
3
Bacterial Zinc Metalloenzyme Inhibitors: Recent Advances and Future Perspectives.
细菌金属锌酶抑制剂：最新进展与未来展望。
Molecules. 2023 May 27;28(11):4378. doi: 10.3390/molecules28114378.
4
Synthesis, Anticancer and Antitubercular Properties of New Chalcones and Their Nitrogen-Containing Five-Membered Heterocyclic Hybrids Bearing Sulfonamide Moiety.新型查耳酮及其含磺酰胺部分的含氮五元杂环杂合体的合成、抗癌和抗结核活性。
Int J Mol Sci. 2022 Oct 20;23(20):12589. doi: 10.3390/ijms232012589.
5
Mutations Reducing Susceptibility to Novel LpxC Inhibitors in and Interplay of Efflux and Nonefflux Mechanisms.突变降低了对新型 LpxC 抑制剂的敏感性 以及外排和非外排机制的相互作用。
Antimicrob Agents Chemother. 2019 Dec 20;64(1). doi: 10.1128/AAC.01490-19.
6
Comparison of three different lipid removal cleanup techniques prior to the analysis of sulfonamide drug residues in porcine tissues.猪组织中磺胺类药物残留分析前三种不同脂质去除净化技术的比较。
Food Sci Nutr. 2019 Aug 7;7(9):3006-3016. doi: 10.1002/fsn3.1158. eCollection 2019 Sep.
7
A pathway-directed positive growth restoration assay to facilitate the discovery of lipid A and fatty acid biosynthesis inhibitors in Acinetobacter baumannii.一种基于通路导向的正向生长恢复检测方法，可促进鲍曼不动杆菌中脂多糖和脂肪酸生物合成抑制剂的发现。
PLoS One. 2018 Mar 5;13(3):e0193851. doi: 10.1371/journal.pone.0193851. eCollection 2018.