Design, synthesis, and pharmacological evaluation of aryl oxadiazole linked 1,2,4-triazine derivatives as anticonvulsant agents
نویسندگان
چکیده
A series of new clubbed aryl oxadiazole-1,2,4-triazine derivatives (6a-l) were designed and synthesized using appropriate chemical routes. The structures to have the required structural elements for any compounds be potential anticonvulsant. Preliminary screening anticonvulsant activity was performed maximal electroshock seizure (MES), subcutaneous pentylenetetrazole-induced (scPTZ) behavioral assessed by motor impairment test actophotometer test. 6-((5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)amino)-1,2,4-triazine-3(2H)-thione (6f) 6-((5-(4-hydroxyphenyl)-1,3,4-oxadiazol-2-yl)amino)-1,2,4-triazine-3(2H)-thione (6g) revealed significant against both MES scPTZ indicating that are effective generalized tonic-clonic absence seizure. lead compound further evaluated quantitative evaluation emerged as most with median dose 28.5 mg/kg (MES ED50), 76.6 toxic (TD50) found >500 mg/kg. In GABA estimation study results showed significantly increased concentration.
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ژورنال
عنوان ژورنال: Medicinal Chemistry Research
سال: 2022
ISSN: ['1554-8120', '1054-2523']
DOI: https://doi.org/10.1007/s00044-022-02880-4