Two novel series of 3,4-dihydroisoquinolin with heterocycle derivatives (4aââ?¬â??t and 9aââ?¬â??e) were\nsynthesized and evaluated for their anticonvulsant activity using maximal electroshock (MES) test and\npentylenetetrazole (PTZ)-induced seizure test. All compounds were characterized by IR, 1H-NMR,\n13C-NMR, and mass spectral data. Among them, 9-(exyloxy)-5,6-dihydro-[1,2,4]triazolo[3,4-a]\nisoquinolin-3(2H)-one (9a) showed significant anticonvulsant activity in MES tests with an ED50 value\nof 63.31 mg/kg and it showed wide margins of safety with protective index (PI > 7.9). It showed much\nhigher anticonvulsant activity than that of valproate. It also demonstrated potent activity against\nPTZ-induced seizures. A docking study of compound 9a in the benzodiazepine (BZD)-binding site\nof Ã?³-aminobutyric acidA (GABAA) receptor confirmed possible binding of compound 9a with the\nBZD receptors.
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