Medicinal Chemistry Research

, Volume 28, Issue 1, pp 52–61 | Cite as

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

  • Zhi-Yang Fu
  • Qing-Hao Jin
  • Ya-Nan Xia
  • Hai-Ying JiangEmail author
  • Li-Ping GuanEmail author
Original Research


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.


Isoquinoline-2(1H)-carboxamide Synthesis Antidepressant Anticonvulsant Neurotransmitter 



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).

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.


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© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Food and Pharmacy CollegeZhejiang Ocean UniversityZhouShanChina
  2. 2.Donghai Science and Technology CollegeZhejiang Ocean UniversityZhoushanChina
  3. 3.College of MedicineJiaxing UniversityJiaxingChina

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