Design and synthesis of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH) as potential antibacterial agents.

Shi L; Fang RQ; Zhu ZW; Yang Y; Cheng K; Zhong WQ; Zhu HL

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design and synthesis of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH) as potential antibacterial agents.

【24h】

Design and synthesis of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH) as potential antibacterial agents.

机译：设计和合成作为潜在抗菌剂的有效的β-酮酰基-酰基载体蛋白合酶III（FabH）抑制剂。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

Twenty new Schiff bases were synthesized by reacting 5-fluoro-salicylaldehyde and primary amine as potent inhibitors of FabH. These compounds were assayed for antibacterial activity against Escherichia coli, Pseudomonas fluorescence, Bacillus subtilis and Staphylococcus aureus. Compounds with potent antibacterial activities were tested for their E. coli FabH inhibitory activity. (E)-4-fluoro-2-((4-hydroxyphenethylimino)methyl)phenol (10) showed the most potent antibacterial activity with MIC of 1.56-6.25 microg/mL against the tested bacterial strains and exhibited the most potent E. coli FabH inhibitory activity with IC(50) of 2.7 microM. Docking simulation was performed to position compound 10 into the E. coli FabH active site to determine the probable binding conformation.

机译：通过使5-氟-水杨醛和作为FabH的有效抑制剂的伯胺反应，合成了二十种新的席夫碱。测定了这些化合物对大肠杆菌，假单胞菌荧光，枯草芽孢杆菌和金黄色葡萄球菌的抗菌活性。测试具有有效抗菌活性的化合物的大肠杆菌FabH抑制活性。（E）-4-氟-2-（（4-羟基苯乙基亚氨基）甲基）苯酚（10）对测试的细菌菌株表现出最强的抗菌活性，MIC为1.56-6.25 microg / mL，并且表现出最强的大肠杆菌FabH抑制活性，IC（50）为2.7 microM。进行对接模拟以将化合物10定位在大肠杆菌FabH活性位点中，以确定可能的结合构象。

著录项

来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第9期|共7页
作者
Shi L; Fang RQ; Zhu ZW; Yang Y; Cheng K; Zhong WQ; Zhu HL;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词

相似文献

外文文献
中文文献
专利

1. Design and synthesis of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH) as potential antibacterial agents. [J] . Shi L, Fang RQ, Zhu ZW, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第9期

机译：设计和合成作为潜在抗菌剂的有效的β-酮酰基-酰基载体蛋白合酶III（FabH）抑制剂。
2. Structure-Based Design,Synthesis,and Study of Potent Inhibitors of beta-Ketoacyl-acyl Carrier Protein Synthase III as Potential Antimicrobial Agents [J] . Zhe Nie, Carin Perretta, Jia Lu, Journal of Medicinal Chemistry . 2005,第5期

机译：基于结构的设计，合成和作为潜在抗菌剂的β-酮酰基-酰基载体蛋白合酶III的有效抑制剂的研究
3. Design, synthesis and antibacterial activities of vanillic acylhydrazone derivatives as potential β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitors [J] . WangX.-L., ZhangY.-B., TangJ.-F., European Journal of Medicinal Chemistry: Chimie Therapeutique . 2012,第Null期

机译：香草酰基hydr衍生物作为潜在的β-酮酰基-酰基载体蛋白合酶III（FabH）抑制剂的设计，合成和抗菌活性
4. Discovering Potent Inhibitors Against the β-Hydroxyacyl-Acyl Carrier Protein Dehydratase (FabZ) of Helicobacter pylori: Structure-Based Design, Synthesis, Bioassay, and Crystal Structure Determination [C] . Lingyan He, Hualiang Jiang, Hong Liu, ICMSI;International conference of molecular simulations and applied informatics technologies . 2010

机译：发现针对幽门螺杆菌的β-羟酰基-酰基载体蛋白脱水酶（FabZ）的有效抑制剂：基于结构的设计，合成，生物测定和晶体结构确定
5. Discovery of novel inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH). [D] . He, Xin. 2002

机译：发现了β-酮酰基-酰基载体蛋白合酶III（FabH）的新型抑制剂。
6. 12-Dithiole-3-Ones as Potent Inhibitors of the Bacterial 3-Ketoacyl Acyl Carrier Protein Synthase III (FabH) [O] . Xin He, Anne McElwee Reeve, Umesh R. Desai, 2004

机译：12-二硫代-3-3作为细菌3-酮酰基酰基载体蛋白合酶III（FabH）的有效抑制剂
7. Synthesis and Antibacterial Activity of Cinnamaldehyde Acylhydrazone with a 1,4-Benzodioxan Fragment as a Novel Class of Potent β-Ketoacyl–Acyl Carrier Protein Synthase III (FabH) Inhibitor [O] . Xiaoda Song, Yushun Yang, Jing Zhao, 2014

机译：用1,4-苯并二氧基丙烯酰基丙烯酰基丙烯酰基的合成和抗菌活性作为一种新型β-酮酰酰基 - 酰基 - 丙烯酰基蛋白合酶III（FABH）抑制剂

Design and synthesis of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH) as potential antibacterial agents.

摘要

著录项

相似文献

相关主题

期刊订阅