Synthesis and Evaluation of the Anticonvulsant Activities of 4-(2-(Alkylthio)benzo[d]oxazol-5-yl)-2,4-dihydro-3H-1,2,4-triazol-3-ones.
Synthesis and Evaluation of the Anticonvulsant Activities of 4-(2-(Alkylthio)benzo[d]oxazol-5-yl)-2,4-dihydro-3H-1,2,4-triazol-3-ones.
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4-(2-(烷硫基)苯并[d]恶唑-5-基)-2,4-二氢-3H-1,2,4-三唑-3-酮类化合物的合成及抗惊厥活性评价
DOI：
10.3390/molecules23040756
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发表时间：
2018-03-25
期刊：
影响因子：
--
通讯作者：
Deng XQ
中科院分区：
文献类型：
--
作者：
Song MX;Wang ZY;He SH;Yu SW;Chen SL;Guo DF;Zhao WH;Deng XQ
In this study, a novel series of 4-(2-(alkylthio)benzo[d]oxazol-5-yl)-2,4-dihydro-3H-1,2,4-triazol-3-ones (4a–m) was designed and synthesized. The anticonvulsant activities of these compounds were evaluated by using the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure models in mice. The neurotoxicity of these compounds was evaluated using the rotarod neurotoxicity test. The majority of compounds showed anti-MES activities at 100 or 300 mg/kg. Compound 4g was considered to be the most promising, based on its potency against MES- and PTZ-induced seizures with ED50 values of 23.7 and 18.9 mg/kg, respectively. The TD50 value of 4g was 284.0 mg/kg, which resulted in a higher protective index (PI = TD50/ED50) value than that of carbamazepine and valproate. In an ELISA test, compound 4g significantly increased the γ-aminobutyric acid (GABA) content in mouse brain. In addition, pretreatment with thiosemicarbazide (an inhibitor of the GABA synthesizing enzyme) significantly decreased the activity of 4g in the MES model, which suggests that the mechanism through which compound 4g elicits its anticonvulsive action is at least in part through increasing the GABA level in the brain.
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影响因子：
7.4
作者：
Huisman, Han;Wynveen, Paul;Kellermann, Gottfried
通讯作者：
Kellermann, Gottfried
影响因子：
3.6
作者：
KATZ, L;COHEN, MS
通讯作者：
COHEN, MS
影响因子：
2.7
作者：
Singh, Sanjay P;Sankaraneni, Ram;Antony, Arun R
通讯作者：
Antony, Arun R
作为潜在抗惊厥药物的新型含杂环 3,4-二氢异喹啉衍生物的合成和药理评价。
DOI：
10.3390/molecules21121635
发表时间：
2016-11-29
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Zhang HJ;Shen QK;Jin CM;Quan ZS
通讯作者：
Quan ZS
影响因子：
1.9
作者：
Tan, Yuede;He, Xiaoyan;Deng, Xianqing
通讯作者：
Deng, Xianqing