Study on synthesis and biological effects of a series of 3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives
| Autor: | Qing-Hao Jin, Ya-Nan Xia, Li-Ping Guan, Zhi-Yang Fu, Hai-Ying Jiang |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
010405 organic chemistry
medicine.drug_class Chemistry medicine.medical_treatment Organic Chemistry Analgesic Central nervous system Carboxamide Pharmacology medicine.disease 01 natural sciences 0104 chemical sciences 010404 medicinal & biomolecular chemistry Anticonvulsant Agent Epilepsy medicine.anatomical_structure Anticonvulsant Mechanism of action medicine Antidepressant General Pharmacology Toxicology and Pharmaceutics medicine.symptom |
| Zdroj: | Medicinal Chemistry Research. 28:52-61 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-018-2261-2 |
| Popis: | In this paper, we have reported the synthesis and biological evaluation of nineteen (S)-N-substituted-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives as novel candidate antidepressant and anticonvulsant agents. Compounds 2h, 2k, 2r, and 2s exhibited better potent antidepressant activity and displayed the antidepressant effects in a dose-dependent manner from 10 to 30 mg/kg in the FST and TST. And, we found that the best antidepressant effect of compounds 2r and 2s are likely mediated by an increase in central nervous system 5-HT and NE. In addition, compounds 2r and 2s also exhibited the anticonvulsant activity against MES-induced seizures. Thus, compounds 2r and 2s may be a useful antidepressant adjunct therapy for treating depression in patients with epilepsy. In addition, compounds 2r and 2s showed the anti-inflammatory activity and the excellent analgesic activity. Several scholars have postulated the anti-inflammatory and analgesic effects of antidepressant drugs, suggesting that they may be possess a similar mechanism of action. |
| Databáze: | OpenAIRE |
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