Metronidazole containing pyrazole derivatives potently inhibit tyrosyl-tRNA synthetase:design,synthe

来源 :第八届国际分子模拟与信息技术应用学术会议 | 被引量 : 0次 | 上传用户：cq2427

【摘要】

：

　　As an important enzyme in bacterial protein biosynthesis,tyrosyl-tRNA synthetase(TyrRS)has been an absorbing therapeutic target tor exploring novel antibact

【作者】

：

Long-WangChen;Peng-FeiWang;Dan-JieTang;Xiang-XiangTao;Ruo-JunMan;Han-YueQiu;Zhong-ChangWang;ChenXu;Hai-LiangZhu;

【机构】

：

State Key Laboratory of Pharmaceutical Bioreclmology,Nanjing University,Nanjing,China

【出处】

：

第八届国际分子模拟与信息技术应用学术会议

【发表日期】

：

2016年期

下载到本地 , 更方便阅读

下载此文赞助VIP

声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架

论文部分内容阅读

　　As an important enzyme in bacterial protein biosynthesis,tyrosyl-tRNA synthetase(TyrRS)has been an absorbing therapeutic target tor exploring novel antibacterial agents.A series of metronidazole-based antibacterial agents has been synthesized and identified as TyrRS inhibitors with low cytotoxicity and significant antibacterial activity,especially against Gram-negative organisms.Of the compounds obtained,4f is the most potent agent which inhibited the growth of Pseudomonas aeruginosa ATCC 13525(MIC = 0.98 μg/mL)and exhibited TryRS inhibitory activity(IC50 = 0.92 μM).Docking simulation was performed to further understand its potency.Membrane-mediated apoptosis in P.aeruginosa was verified by flow cytometry.

其他文献

Synthesis,Molecular Modeling,and Biological Evaluation of Novel 1,3-Diphenyl-2-propen-1-one Based Py

　　A novel series of 1,3-diphenyl-2-propen-1-one(chalcone)derivatives was synthesized by a simple,ecofriendly,and efficient Claisen-Schmidt condensation reacti

会议

Synthesis and biological evaluation of novel aryl-2H-pyrazole derivatives as potent non-purine xanth

　　A series of aryl-2H-pyrazole derivatives were synthesized and evaluated for inhibitory activity against xanthine oxidase in vitro as potent xanthine oxidase

会议

Synthesis,biological evaluation and molecular modeling of 1H-benzo[d]imidazole derivatives as novel

　　A series of novel compounds(8a-21b)were designed and synthesized based on lH-benzo[d]imidazole.Their biological activities were evaluated as potential tubul

会议

Synthesis and antibacterial evaluation of novel Schiff's base derivatives of nitroimidazole nuc

　　Series of novel Schiff's base derivatives have been synthesized by combining 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl 4-formylbenzoate 5,6 with aromatic/h

会议

Synthesis and Biological Evaluation of 1-Methyl-1H-indole-Pyrazoline Hybrids as Potential Tubulin Po

　　A series of 1-methyl-1H-indole-pyrazoline hybrids were designed,synthesized,and biologically evaluated as potential tubulin polymerization inhibitors.Among

会议

Synthesis and biological evaluation of novel indole derivatives containing sulfonamide scaffold as p

　　Microtubule-targeted drugs play a critical role in various types of cancer therapy worldwide.In our study,a series of novel indole derivatives containing su

会议

Navigating into the chemical space between MGCD0103 and SAHA:novel histone deacetylase inhibitors as

　　Histone deacetylase inhibitors(HDIs)are an increasingly important class of cancer-targeting agent.Two kinds of small molecule histone deacetylase inhibitors

会议

Synthesis,biological evaluation and molecular docking studies of novel l-(4,5-dihydro-lH-pyrazol-1-y

　　A series of novel compounds(6a-6v)containing l-methylindol and 31-(4,5-dihydro-lH-pyraxol-1-yl)ethanone skeleton were designed,synthesized and biologically

会议

Inflammatory pathway network-based drug repositioning and molecular phenomics

会议

Predicting cancer-relevant proteins using an improved molecular similarity ensemble approach

　　In this study,we proposed an improved algorithm for identifying proteins relevant to cancer.The algorithm was named two-layer molecular similarity ensemble

会议

Metronidazole containing pyrazole derivatives potently inhibit tyrosyl-tRNA synthetase:design,synthe

其他学术论文