Central Nervous System Agents in Medicinal Chemistry published new progress about Anticonvulsants. 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, Name: Methyl 2,3-dichlorobenzoate.
Verma, Krishan K.; Singh, Umesh K.; Jain, Jainendra published the artcile< Screening of Some Novel 4, 5 Disubstituted 1, 2, 4-Triazole-3-thiones for Anticonvulsant Activity>, Name: Methyl 2,3-dichlorobenzoate, the main research area is triazole thione anticonvulsant drug screening; GABA-AT; MES; Triazol-3-thiones; anticonvulsant activity; docking; scPTZ..
In the present study, we synthesized fifteen 4, 5-disubstituted 1, 2, 4-triazol- 3-thione derivatives and evaluated for anticonvulsant activity with neurotoxicity determination The synthesized compounds were characterized using FTIR, 1H-NMR and MS. The mol. docking study was also performed to study the interactions of compounds with LYS329 residue of gamma amino butyric acid aminotransferase (GABA-AT) using Autodock 4.2 software. The anticonvulsant activity was assessed by maximal electroshock (MES) test and s.c. pentylenetetrazol (scPTZ) tests. The neurotoxicity was assessed by rotarod ataxia test. In MES test, compounds 5a, 8a and 9a were found active at 100 mg/kg and five compounds were found active at 300 mg/kg dose after 1 h of administration. After 4 h of drug administration, only two compounds 8a and 9a exhibited protection at 100 mg/kg. In scPTZ test, three compounds 2a, 6a and 8a were found active at 100 mg/kg and 7a was active at 300 mg/kg after 1 h of test drug administration. Most of the compounds were found active in MES test with 8a and 9a being the most active among all. In docking study, 2a was found to be best compound based on the binding energy of -6.5 kcal/mol and estimated inhibition constant of 17.2μM. Majority of synthesized compounds were found active in MES test, whereas only few were found to possess anti scPTZ activity. Among all compounds, only 14a caused motor coordination impairment in rotarod ataxia test at 300 mg/kg 1 h duration.
Central Nervous System Agents in Medicinal Chemistry published new progress about Anticonvulsants. 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, Name: Methyl 2,3-dichlorobenzoate.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics