Practical Synthesis, Antidepressant, and Anticonvulsant Activity of 3-Phenyliminoindolin-2-one Derivatives
| Autor: | Xue-Wu Zhang, Xing-Hua Zhen, Li-Ping Guan, Hong-Guo Jin, Jian-Yin Ma, Ying-Chun Quan |
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| Rok vydání: | 2015 |
| Předmět: |
Spectrometry
Mass Electrospray Ionization Indoles Metabolite medicine.medical_treatment Proton Magnetic Resonance Spectroscopy Pharmacology 01 natural sciences Biochemistry Medicinal chemistry 03 medical and health sciences chemistry.chemical_compound Mice 0302 clinical medicine Drug Discovery medicine Animals 010405 organic chemistry Chemistry Organic Chemistry Neurotoxicity medicine.disease Tail suspension test Antidepressive Agents 0104 chemical sciences Anticonvulsant Indoline Molecular Medicine Antidepressant Anticonvulsants Serotonin 030217 neurology & neurosurgery Behavioural despair test |
| Zdroj: | Chemical biologydrug design. 87(3) |
| ISSN: | 1747-0285 |
| Popis: | Herein, a series of 3-phenyliminoindolin-2-one derivatives were designed, synthesized, and screened for their antidepressant and anticonvulsant activities. The IR spectra of the compounds afforded NH stretching (3340-3346 cm(-1)) bands and C=O stretching (1731-1746 cm(-1)). In the (1)H-NMR spectra of the compounds, N-H protons of indoline ring were observed at 10.65-10.89 ppm generally as broad bands, and (13)C-NMR spectra of the compounds C=O were seen at 161.72-169.27 ppm. Interestingly, compounds 3o, 3p and 3r significantly shortened immobility time in the The forced swimming test (FST) and The tail suspension test (TST) at 50 mg/kg dose levels. In addition, compound 3r exhibited higher levels of efficacy than the reference standard fluoxetine but had no effect on locomotor activity in the open-field test. Compound 3r significantly increased serotonin and norepinephrine and the metabolite 5-hydroxyindoleacetic acid in mouse brain, suggesting that the effects of compound 3r may be mediated through these neurotransmitters. In the seizure screen, 15 compounds showed some degree against PTZ-induced seizure at a dose of 100 mg/kg, and the tested compounds did not show any neurotoxicity at a dose of 300 mg/kg in the rotarod test. |
| Databáze: | OpenAIRE |
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