Synthesis, characterization & anticonvulsant activity of amide derivatives of 4-amino-1,2-naphthoquinone
作者:Mukesh Bansal、Bharat Goel、Shubhanjali Shukla、Radhey Shyam Srivastava
DOI:10.1007/s00044-013-0531-6
日期:2013.11
spectroscopic (FT-IR, 1H NMR and 13C NMR) and elemental analysis. The synthesized compounds were evaluated for anticonvulsant activity by the maximal electroshock (MES) test and subcutaneous pentylenetetrazole (sc. PTZ) test, the most widely employed seizure models for early identification of anticonvulsant candidates, whereas their neurotoxicity was examined by rotarod test. Compounds were administered to animals
在本研究中,合成了4-氨基-1,2-萘醌类似物,并通过光谱(FT-IR,1 H NMR和13 C NMR)和元素分析对其进行了表征。通过最大电休克(MES)试验和皮下戊二烯四唑(sc。PTZ)试验评估了合成的化合物的抗惊厥活性,这是最广泛使用的癫痫发作模型,可早期鉴定抗惊厥候选药物,而其神经毒性则通过rotarod试验进行了检验。通过腹膜内(ip)途径将化合物以不同的浓度(10、20和40 mg / kg)施用给动物,并测量了癫痫发作的保护百分比。药理结果表明,大多数化合物对MES和sc有效。云台测试。化合物N-(1,2-二氢-1,2-二氧杂萘-4-基)丁酰胺(4)和N-(1,2-二氢-1,2-二氧杂萘-4-基)-3-甲基丁酰胺(6)分别以40和20 mg / kg的剂量具有活性,而化合物N-(1,2-二氢-1,2-二氧杂萘-4-基)己酰胺(7)和4-乙酰氨基-N-(1,2-二氢-1,2-