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Exploration of the structure-activity relationship and druggability of novel oxazolidinone-based compounds as Gram-negative antibacterial agents

文献类型：期刊论文

作者Ding, Shi1,2; Ji, Jing-Chao2; Zhang, Ming-Juan2; Yang, Yu-She1; Wang, Rui3; Zhu, Xing-Long2; Wang, Li-Hong2; Zhong, Yi2; Gao, Le2; Lu, Man2
刊名ARCHIV DER PHARMAZIE
出版日期2019-09-03
页码13
关键词antibacterial activity oxazolidine QSAR
ISSN号0365-6233
DOI10.1002/ardp.201900129
通讯作者Liu, Ju(liuju1216@126.com) ; Chen, Ye(sy-chenye@163.com)
英文摘要To gain further knowledge of the structure-activity relationship and druggability of novel oxazolidinone-based UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) inhibitors as Gram-negative antibacterial agents, compounds containing the hydrophobic tails with different lengths and terminal substitutions were synthesized and their antibacterial activities against standard and clinically isolated Gram-negative strains were evaluated. We summarized their structure-activity relationships and found that oxazolidinone-based compounds exhibited a narrower antibacterial spectrum compared with threonine-based compounds. Furthermore, we parallelly compared the metabolic stabilities of the compounds with the classic threonine scaffold and the novel oxazolidinone scaffold in liver microsomes. The results indicated that the druggability of the oxazolidinone scaffold may be inferior to the classic threonine scaffold in the design of LpxC inhibitors.
WOS关键词LPXC INHIBITORS ; BIOLOGICAL EVALUATION ; ANTIBIOTIC-ACTIVITY ; DEACETYLASE LPXC ; DESIGN
资助项目Youth Project of Education Department of Liaoning Province[LQN201709] ; National Natural Science Foundation of China[21807055]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000484857800001
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/288595]  
专题新药研究国家重点实验室
通讯作者Liu, Ju; Chen, Ye
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China
2.Liaoning Univ, Coll Pharm, Key Lab New Drug Res & Dev Liaoning Prov, Shenyang, Liaoning, Peoples R China
3.Shenyang Med Coll, Cent Hosp, Shenyang, Liaoning, Peoples R China
推荐引用方式
GB/T 7714		 Ding, Shi,Ji, Jing-Chao,Zhang, Ming-Juan,et al. Exploration of the structure-activity relationship and druggability of novel oxazolidinone-based compounds as Gram-negative antibacterial agents[J]. ARCHIV DER PHARMAZIE,2019:13.
APA Ding, Shi.,Ji, Jing-Chao.,Zhang, Ming-Juan.,Yang, Yu-She.,Wang, Rui.,...&Chen, Ye.(2019).Exploration of the structure-activity relationship and druggability of novel oxazolidinone-based compounds as Gram-negative antibacterial agents.ARCHIV DER PHARMAZIE,13.
MLA Ding, Shi,et al."Exploration of the structure-activity relationship and druggability of novel oxazolidinone-based compounds as Gram-negative antibacterial agents".ARCHIV DER PHARMAZIE (2019):13.

入库方式： OAI收割

来源：上海药物研究所

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