Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents

doi:10.1016/j.ejmech.2019.03.059

	Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents
	Liu, Hongyan 1; Sun, Danwen 4; Du, Hang 1; Zheng, Changji 1; Li, Jingya 3; Piao, Huri 1; Li, Jia 3; Sun, Liangpeng 1,2
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2019-06-15
卷号	172 页码:163-173
关键词	Tryptophan-derived rhodanine PTP1B inhibitor Anti-bacterial SAR
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2019.03.059
通讯作者	Piao, Huri(piaohr@ybu.edu.cn) ; Li, Jia(jli@simm.ac.cn) ; Sun, Liangpeng(lpsun@ybu.edu.cn)
英文摘要	Several series of novel tryptophan-derived rhodanine derivatives were synthesized and identified as potential competitive PTP1B inhibitors and antibacterial agents. Among the compounds studied, 10b was found to have the best in vitro inhibition activity against PTP1B (IC50= 0.36 +/- 0.02 mu M). In addition, the compounds also showed potent inhibition against other PTPs, especially CDC25B. Molecular docking analysis demonstrated that compounds 7c and 10b could occupy both the catalytic site and the adjacent pTyr binding site simultaneously. The compounds also showed higher levels of activity against gram-positive strains, the gram-negative strain Escherichia coli 1924, and multidrug-resistant gram-positive bacterial strains. Compounds 7c, 8c, 9e, 10a, and 10c had comparable or more potent antibacterial activity than the positive controls. (C) 2019 Elsevier Masson SAS. All rights reserved.
资助项目	National Natural Science Foundation of China[81460524] ; National Natural Science Foundation of China[81360473] ; National Natural Science Foundation of China[81125023] ; Education Department of Jilin Province Scientific Research Fund Project[2015-50] ; Edanz Group China
WOS关键词	TYROSINE-PHOSPHATASE 1B ; INSULIN-RECEPTOR ; PROTEIN ; ACID ; DISCOVERY ; OBESITY ; POTENT ; SENSITIVITY
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:000466828400013
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/289925]
专题	中国科学院上海药物研究所
通讯作者	Piao, Huri; Li, Jia; Sun, Liangpeng
作者单位	1.Yanbian Univ, Coll Pharm, Minist Educ, Key Lab Nat Resources Changbai Mt & Funct Mol, Yanji 133000, Peoples R China 2.Yanbian Univ, Coll Med, Yanji 133000, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 4.East China Normal Univ, Coll Chem & Mol Engn, 3663 Zhongshan North Rd, Shanghai 200062, Peoples R China
推荐引用方式 GB/T 7714	Liu, Hongyan,Sun, Danwen,Du, Hang,et al. Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2019,172:163-173.
APA	Liu, Hongyan.,Sun, Danwen.,Du, Hang.,Zheng, Changji.,Li, Jingya.,...&Sun, Liangpeng.(2019).Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,172,163-173.
MLA	Liu, Hongyan,et al."Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 172(2019):163-173.