Study on synthesis and biological effects of a series of 3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives
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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.
KeywordsIsoquinoline-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).
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Conflict of interest
The authors declare that they have no conflict of interest.
- D’Angelo V, Tessari F, Bellagamba G, De Luca E, Cifelli R, Celia C, Primavera R, Di Francesco M, Paolino D, Di Marzio L, Locatelli M (2016) Microextraction by packed sorbent and HPLC-PDA quantification of multiple anti-inflammatory drugs and fluoroquinolones in human plasma and urine. J Enzym Inhib Med Chem 31(sup3):110–116CrossRefGoogle Scholar
- Gaidukevich SK, Mikulovich YL, Smirnova TG, Andreevskaya SN, Sorokoumova GM, Chernousova LN, Selishcheva AA, Shvets VI (2016) Antibacterial effects of liposomes containing phospholipid cardiolipin and fluoroquinolone levofloxacin on mycobacterium tuberculosis with extensive drug resistance. Bull Exp Biol Med 160:675–678CrossRefGoogle Scholar
- McNamara JO (2011) Pharmacotherapy of the epilepsies. In: Brunton LL, Chabner BA, Knollmann BC (Eds.). Goodman & Gilman’s the phamacological basis of therapeutics, twelfth edn. McGraw-Hill, New York, NY, p 583–608Google Scholar
- Porsolt RD, Bertin A, Jalfre M (1997) Behavioural despair in mice: a primary screening test for antidepressants. Arch Int Pharmacodyn 229:327–336Google Scholar
- Uddin MMN, Kabir MSH, Hasan M, Al Mahmud Z, Alam Bhuiya NMM, Ahmed F, Hasan MR, Hosen MT, Alam MS (2018) Assenssment of the antioxidant, thrombolytic, analgesic, anti-inflammatory, antidepressant and anxiolytic activities of leaf extracts and fractions of Tetracera sarmentosa (L.) Vahl. J Basic Clin Physiol Pharmacol 29:81–93CrossRefGoogle Scholar