Synthesis and evaluation of anticonvulsant and antidepressant activities of 5-alkoxytetrazolo[1,5-c]thieno[2,3-e]pyrimidine derivatives
Synthesis and evaluation of anticonvulsant and antidepressant activities of 5-alkoxytetrazolo[1,5-c]thieno[2,3-e]pyrimidine derivatives
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5-烷氧基四唑并[1,5-c]噻吩并[2,3-e]嘧啶衍生物的合成及抗惊厥和抗抑郁活性评价。
DOI：
10.1016/j.ejmech.2012.08.027
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发表时间：
2012-10-01
影响因子：
6.7
通讯作者：
Guan, Li-Ping
中科院分区：
文献类型：
--
作者：
Wang, Shi-Ben;Deng, Xian-Qing;Guan, Li-Ping
合成了一系列5-烷氧四唑[1,5-c]噻吩[2,3-e]嘧啶衍生物，并对其抗惊厥和抗抑郁活性进行了评价。药理试验表明，合成的化合物中有4种具有较弱的抗惊厥活性，而大多数化合物具有良好的抗抑郁活性。活性最强的化合物为5-（2,4-二氯双酶氧基）四唑[1,5-c]噻吩[2,3-e]嘧啶，在100 mg/kg剂量下可使固定时间缩短51.62%。野外实验结果表明，与对照组相比，该化合物在强迫游泳试验中测定的剂量对运动活动没有显著影响。这意味着在FST中检测到的抗抑郁活性不是中枢神经系统兴奋特性的结果，并进一步证实了其抗抑郁样作用。(C) 2012 Elsevier Masson SAS。版权所有。
A series of 5-alkoxytetrazolo[1,5-c]thieno[2,3-e]pyrimidine derivatives were synthesized and their anticonvulsant and antidepressant activities were evaluated. Pharmacological tests showed that four of the synthesized compounds had weak anticonvulsant activity, while most of the compounds had excellent antidepressant activity. The most active compound was 5-(2,4-dichlorobenzyloxy)tetrazolo [1,5-c] thieno[2,3-e]pyrimidine, which decreased the immobility time by 51.62% at a dose of 100 mg/kg. The results of open-field tests of this compound indicated that it had no significant effects on the locomotor activity compared with the control group at the doses assayed in the forced swimming tests test. This means that the antidepressant activity detected in the FST for the compound is not the result of central nervous system stimulant properties, and further confirms its antidepressant-like effect. (C) 2012 Elsevier Masson SAS. All rights reserved.