Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects
| Autor: | Zhi-Yang Fu, Qing-Hao Jin, Hai-Ying Jiang, Li-Ping Guan |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Male
Aquatic Organisms synthesis medicine.medical_treatment Drug Evaluation Preclinical Pharmaceutical Science Pharmacology Mice Drug Discovery lcsh:QH301-705.5 Pharmacology Toxicology and Pharmaceutics (miscellaneous) ED50 Electroshock Mice Inbred ICR Depression Chemistry Antidepressive Agents Treatment Outcome Antidepressant Anticonvulsants anticonvulsant Injections Intraperitoneal medicine.drug Antarctic Regions antarctic-derived fungus Article Norepinephrine (medication) Seizures Fluoxetine Toxicity Tests medicine Animals Humans Benzothiazoles benzo[d]thiazol antidepressant Biological Products Dose-Response Relationship Drug Valproic Acid Penicillium Disease Models Animal Anticonvulsant lcsh:Biology (General) Phenobarbital Serotonin Stress Psychological Behavioural despair test |
| Zdroj: | Marine Drugs; Volume 17; Issue 7; Pages: 430 Marine Drugs, Vol 17, Iss 7, p 430 (2019) Marine Drugs |
| ISSN: | 1660-3397 |
| DOI: | 10.3390/md17070430 |
| Popis: | Thirty-four new benzo[d]thiazol derivatives 2a−2i, 3a−3r, and 4a−4g were synthesized and investigated for their potential antidepressant and anticonvulsant effects. In a forced swimming test, 2c and 2d showed the highest antidepressant and anticonvulsant effects. 2c and 2d displayed a higher percentage decrease in immobility duration (89.96% and 89.62%, respectively) than that of fluoxetine (83.62%). In the maximal electroshock seizure test, 3n and 3q showed the highest anticonvulsant effect, with ED50 values of 46.1 and 64.3 mg kg−1, and protective indices of 6.34 and 4.11, respectively, which were similar to those of phenobarbital or valproate. We also found that the mechanism for the antidepressant activity of 2c and 2d may be via increasing the concentrations of serotonin and norepinephrine. |
| Databáze: | OpenAIRE |
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