TY - JOUR ID - 88821 TI - Design, Synthesis and Biological Evaluation of Benzo[D]Thiazole with Dimethylpyrazol Derivatives JO - Asian Pacific Journal of Cancer Prevention JA - APJCP LA - en SN - 1513-7368 AU - Liu, Dachuan AU - Cheng, Xiu AU - Wang, Ying AD - School of Pharmacy, Bengbu Medical College, Bengbu, China. AD - School of Public Foundation, Bengbu Medical College, Bengbu, China. Y1 - 2019 PY - 2019 VL - 20 IS - 11 SP - 3487 EP - 3495 KW - Benzothiazole KW - Dimethylpyrazol KW - Maximal Electroshock KW - MTT assay, GABAergic DO - 10.31557/APJCP.2019.20.11.3487 N2 - A series of new benzothiazole derivatives containing dimethylpyrazole 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 (6a, 6b, 6g and 6m) 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 showed lower neurotoxicity and little cytotoxicity, so that the compounds, which with better activities, also had higher protective index. In particular, the compound 6g, 2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-((2-fluorobenzyl)oxy)benzo[d]thiazole 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 positive controls in this study. After that the compound 6g demonstrated antagonistic activity against seizures induced by pentylenetetrazol, which proved 6g maybe exert activity through effecting GABAergic neurotransmission.   UR - https://journal.waocp.org/article_88821.html L1 - https://journal.waocp.org/article_88821_6cc22692ce6a39412c22a7e78d89de41.pdf ER -