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Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents
- Source :
- European Journal of Medicinal Chemistry. 172:163-173
- Publication Year :
- 2019
- Publisher :
- Elsevier BV, 2019.
-
Abstract
- 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 μM). 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.
- Subjects :
- Rhodanine
Microbial Sensitivity Tests
medicine.disease_cause
01 natural sciences
Structure-Activity Relationship
03 medical and health sciences
chemistry.chemical_compound
Drug Resistance, Multiple, Bacterial
Drug Discovery
medicine
Enzyme Inhibitors
Binding site
Escherichia coli
030304 developmental biology
Biological evaluation
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Pharmacology
0303 health sciences
Dose-Response Relationship, Drug
Molecular Structure
Strain (chemistry)
010405 organic chemistry
Organic Chemistry
Tryptophan
General Medicine
Anti-Bacterial Agents
0104 chemical sciences
chemistry
Biochemistry
Anti bacterial
Antibacterial activity
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 172
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....d4018792fc37ef36dd8bb727b47e1dd0