Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria
文献类型：期刊论文
| 作者 | Yang, Shouning1; Shi, Wei1; Xing, Dong1; Zhao, Zheng2; Lv, Fengping1; Yang, Liping1; Yang, Yushe3 ; Hu, Wenhao1,3
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2014-10-30 |
| 卷号 | 86页码:133-152 |
| 关键词 | Drug resistant bacteria Peptide deformylase inhibitor Proline derivatives |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2014.07.106 |
| 文献子类 | Article |
| 英文摘要 | Peptide deformylase (PDF) has been identified as a promising target for novel antibacterial agents. In this study, a series of novel formyl hydroxyamino derivatives were designed and synthesized as PDF inhibitors and their antibacterial activities were evaluated. Among the potent PDF inhibitors (1o, 1q, 1o', 1q', and 1x), in vivo studies showed that compound 1q possesses mild toxicity, a good pharmacokinetic profile and protective effects. The good in vivo efficacy and low toxicity suggest that this class of compounds has potential for development and use in future antibacterial drugs. (c) 2014 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | SIDE-CHAIN ; PHARMACOKINETICS ; BB-3497 ; LBM415 ; ACTINONIN ; TARGET ; AGENTS ; MODEL |
| 资助项目 | NSF of China[21125209] ; NSF of China[21332003] ; MOST of China[2011CB808600] ; STCSM[12JC1403800] ; State Key Laboratory of Drug Research[SIMM1403KF-09] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000343781800015 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276862]  |
| 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 | Hu, Wenhao |
| 作者单位 | 1.E China Normal Univ, Dept Chem, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China; 2.E China Normal Univ, Minist Educ, Shanghai Key Lab Brain Funct Genom, Key Lab Brain Funct Genom, Shanghai 200062, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Shouning,Shi, Wei,Xing, Dong,et al. Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,86:133-152. |
| APA | Yang, Shouning.,Shi, Wei.,Xing, Dong.,Zhao, Zheng.,Lv, Fengping.,...&Hu, Wenhao.(2014).Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,86,133-152. |
| MLA | Yang, Shouning,et al."Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 86(2014):133-152. |
入库方式： OAI收割
来源：上海药物研究所
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