Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria

doi:10.1016/j.ejmech.2014.07.106

	Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria
	Yang, Shouning 1; Shi, Wei 1; Xing, Dong 1; Zhao, Zheng 2; Lv, Fengping 1; Yang, Liping 1; Yang, Yushe3 ; Hu, Wenhao 1,3
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	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.
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关键词	SIDE-CHAIN ; PHARMACOKINETICS ; BB-3497 ; LBM415 ; ACTINONIN ; TARGET ; AGENTS ; MODEL
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:000343781800015
内容类型	期刊论文
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.