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

被引：14

作者：

Yang, Shouning ^{[1
]}

Shi, Wei ^{[1
]}

Xing, Dong ^{[1
]}

Zhao, Zheng ^{[2
]}

Lv, Fengping ^{[1
]}

Yang, Liping ^{[1
]}

Yang, Yushe ^{[3
]}

Hu, Wenhao ^{[1
,3
]}

机构：

[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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 86卷

关键词：

Drug resistant bacteria; Peptide deformylase inhibitor; Proline derivatives; SIDE-CHAIN; PHARMACOKINETICS; BB-3497; LBM415; ACTINONIN; TARGET; AGENTS; MODEL;

D O I：

10.1016/j.ejmech.2014.07.106

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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.

引用

页码：133 / 152

页数：20

共 46 条

[1] ON RELEASE OF FORMYL GROUP FROM NASCENT PROTEIN [J].