Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents
文献类型：期刊论文
| 作者 | Liu, Hongyan1; Sun, Danwen4; Du, Hang1; Zheng, Changji1; Li, Jingya3 ; Piao, Huri1; Li, Jia3; Sun, Liangpeng1,2
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 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. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; INSULIN-RECEPTOR ; PROTEIN ; ACID ; DISCOVERY ; OBESITY ; POTENT ; SENSITIVITY |
| 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研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000466828400013 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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