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Study on synthesis and biological effects of a series of 3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives

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Abstract

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.

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Acknowledgements

This research was funded by the National Natural Science Foundation of China (No. 81560149) and 13th Five-Year Key Projects of Jilin Provincial Education Department of China (No. JJKH2016261H).

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Authors and Affiliations

  1. Food and Pharmacy College, Zhejiang Ocean University, 316022, ZhouShan, Zhejiang, China

    Zhi-Yang Fu, Ya-Nan Xia & Li-Ping Guan

  2. Donghai Science and Technology College, Zhejiang Ocean University, 316000, Zhoushan, Zhejiang, China

    Qing-Hao Jin

  3. College of Medicine, Jiaxing University, 314001, Jiaxing, Zhejiang, China

    Hai-Ying Jiang

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  1. Zhi-Yang Fu
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  2. Qing-Hao Jin
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  3. Ya-Nan Xia
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Correspondence to Hai-Ying Jiang or Li-Ping Guan.

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Fu, ZY., Jin, QH., Xia, YN. et al. Study on synthesis and biological effects of a series of 3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives. Med Chem Res 28, 52–61 (2019). https://doi.org/10.1007/s00044-018-2261-2

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