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Molecules 2016, 21(12), 1635; doi:10.3390/molecules21121635

Synthesis and Pharmacological Evaluation of New 3,4-Dihydroisoquinolin Derivatives Containing Heterocycle as Potential Anticonvulsant Agents

Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002, China
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 2 November 2016 / Accepted: 25 November 2016 / Published: 29 November 2016
(This article belongs to the Section Medicinal Chemistry)
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Two novel series of 3,4-dihydroisoquinolin with heterocycle derivatives (4at and 9ae) were synthesized and evaluated for their anticonvulsant activity using maximal electroshock (MES) test and pentylenetetrazole (PTZ)-induced seizure test. All compounds were characterized by IR, 1H-NMR, 13C-NMR, and mass spectral data. Among them, 9-(exyloxy)-5,6-dihydro-[1,2,4]triazolo[3,4-a]isoquinolin-3(2H)-one (9a) showed significant anticonvulsant activity in MES tests with an ED50 value of 63.31 mg/kg and it showed wide margins of safety with protective index (PI > 7.9). It showed much higher anticonvulsant activity than that of valproate. It also demonstrated potent activity against PTZ-induced seizures. A docking study of compound 9a in the benzodiazepine (BZD)-binding site of γ-aminobutyric acidA (GABAA) receptor confirmed possible binding of compound 9a with the BZD receptors. View Full-Text
Keywords: synthesis; isoquinoline; anticonvulsant; MES; molecular docking synthesis; isoquinoline; anticonvulsant; MES; molecular docking

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Zhang, H.-J.; Shen, Q.-K.; Jin, C.-M.; Quan, Z.-S. Synthesis and Pharmacological Evaluation of New 3,4-Dihydroisoquinolin Derivatives Containing Heterocycle as Potential Anticonvulsant Agents. Molecules 2016, 21, 1635.

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