Liu, Dachuan; Cheng, Xiu; Wang, Ying published the artcile< Design, synthesis and biological evaluation of benzo[d]thiazole with dimethylpyrazole derivatives>, Application of C7H6Cl2, the main research area is dimethylpyrazolyl benzothiazole preparation antitumor anticonvulsant SAR neurotoxicity; Benzothiazole; Dimethylpyrazol; MTT assay, GABAergic; Maximal Electroshock.
A series of new benzothiazole derivatives containing dimethylpyrazole I [R = H, n-pentyl, benzyl, etc.] were synthesized and evaluated for their anticonvulsant activity, neurotoxicity and cytotoxicity by using the maximal electroshock (MES), rotarod neurotoxicity (TOX) and MTT colorimetric assay. Among the compounds studied, four compounds I [R = Bu, n-pentyl, 2-fluorobenzyl, 2,6-dichlorobenzyl] showed better anticonvulsant than the others at 300 mg/kg and they also showed anticonvulsant activity at the dose of 100 mg/kg. All the synthetic compounds I showed lower neurotoxicity and little cytotoxicity, so that the compounds, which with better activities, also had higher protective index. In particular, the compound I [R = 2-fluorobenzyl] showed better activity with an ED50 value of 160.4 mg/kg and higher protective index (PI) values of 2.74 in the MES test than the standard drugs sodium valproate, which used as pos. controls in this study. After that the compound I [R = 2-fluorobenzyl] demonstrated antagonistic activity against seizures induced by pentylenetetrazol, which proved compound I [R = 2-fluorobenzyl] may be exert activity through effecting GABAergic neurotransmission.
Asian Pacific Journal of Cancer Prevention published new progress about Anticonvulsants. 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Application of C7H6Cl2.
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