Exploration of the structure-activity relationship and druggability of novel oxazolidinone-based compounds as Gram-negative antibacterial agents | |
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 |
2019-09-03 | |
页码 | 13 |
关键词 | antibacterial activity oxazolidine QSAR |
ISSN号 | 0365-6233 |
DOI | 10.1002/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. |
资助项目 | Youth Project of Education Department of Liaoning Province[LQN201709] ; National Natural Science Foundation of China[21807055] |
WOS关键词 | LPXC INHIBITORS ; BIOLOGICAL EVALUATION ; ANTIBIOTIC-ACTIVITY ; DEACETYLASE LPXC ; DESIGN |
WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
语种 | 英语 |
出版者 | WILEY-V C H VERLAG GMBH |
WOS记录号 | WOS:000484857800001 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.183/handle/2S10ELR8/288595] |
专题 | 中国科学院上海药物研究所 |
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. |
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