期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 172, 期 -, 页码 163-173出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.03.059
关键词
Tryptophan-derived rhodanine; PTP1B inhibitor; Anti-bacterial; SAR
资金
- National Natural Science Foundation of China [81460524, 81360473, 81125023]
- Education Department of Jilin Province Scientific Research Fund Project [2015-50]
- Edanz Group China
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.
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