{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,6]],"date-time":"2026-07-06T23:10:33Z","timestamp":1783379433649,"version":"3.54.6"},"reference-count":33,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2016,11,29]],"date-time":"2016-11-29T00:00:00Z","timestamp":1480377600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81360468"],"award-info":[{"award-number":["81360468"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81160409"],"award-info":[{"award-number":["81160409"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Two novel series of 3,4-dihydroisoquinolin with heterocycle derivatives (4a\u2013t and 9a\u2013e) 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 &gt; 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 \u03b3-aminobutyric acidA (GABAA) receptor confirmed possible binding of compound 9a with the BZD receptors.<\/jats:p>","DOI":"10.3390\/molecules21121635","type":"journal-article","created":{"date-parts":[[2016,11,29]],"date-time":"2016-11-29T10:09:48Z","timestamp":1480414188000},"page":"1635","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":15,"title":["Synthesis and Pharmacological Evaluation of New 3,4-Dihydroisoquinolin Derivatives Containing Heterocycle as Potential Anticonvulsant Agents"],"prefix":"10.3390","volume":"21","author":[{"given":"Hong-Jian","family":"Zhang","sequence":"first","affiliation":[{"name":"Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qing-Kun","family":"Shen","sequence":"additional","affiliation":[{"name":"Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chun-Mei","family":"Jin","sequence":"additional","affiliation":[{"name":"Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhe-Shan","family":"Quan","sequence":"additional","affiliation":[{"name":"Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2016,11,29]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"1212","DOI":"10.1046\/j.1528-1157.2001.22001.x","article-title":"Glossary of descriptive terminology for ictal semiology: Report of the ILAE task force on classification and terminology","volume":"42","author":"Blume","year":"2001","journal-title":"Epilepsia"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"464","DOI":"10.1111\/epi.13294","article-title":"Health and economic benefits of public financing of epilepsy treatment in India: An agent-based simulation model","volume":"57","author":"Megiddo","year":"2016","journal-title":"Epilepsia"},{"key":"ref_3","doi-asserted-by":"crossref","first-page":"333","DOI":"10.1016\/j.molstruc.2016.10.052","article-title":"Design, synthesis, molecular modeling and biological evaluation of novel 2,3-dihydrophthalazine-1,4-dione derivatives as potential anticonvulsant agents","volume":"1130","author":"Ayyad","year":"2017","journal-title":"J. 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