Medicinal Chemistry Laboratory, U.C.P.Sc., Kakatiya University, Wararagal, 506009, Telangana, India.
Adv Exp Med Biol. 2017;988:39-48. doi: 10.1007/978-3-319-56246-9_3.
The new heterocyclic compounds are used to treat epilepsy. In the present work new indole derivatives i.e. 5-[2(3)-di alkyl amino alkoxy] Indole 2,3-di-one derivatives are synthesized and characterized and these compounds was subjected to acute toxicity and then screened for antiepileptic activity on Maximal Electroshock (MES) seizures model in albino wistar rats. In that study 5-[2-dimethyl amino ethoxy] Indole 2,3 dione and 5-[2-dimethyl amino ethoxy] Indole 2-one,3-semicarbazone(IVa) showed good antiepileptic activity and less neurotoxicity compared to phenytoin. The purpose of the present study is to investigate the effect of 5-[2-dimethyl amino ethoxy] Indole 2,3-di one and 5-[2-dimethyl amino ethoxy] Indole 2-one,3-semicarbazone(IVa) derivatives on biogenic amines concentrations in rat brain after induction of seizures by Maximal Electro Shock(MES) method. Our aim of study was relationship between seizure activities and altered the monoamines such as noradrenaline (NA), dopamine (DA), serotonin (5-HT) in forebrain of rats in MES seizure models. In MES model, study of 5-[2-dimethyl amino ethoxy] Indole 2,3 dione(IIIa) and 5-[2-dimethyl amino ethoxy] Indole 2-one,3-semicarbazone(IVa) (100 mg/kg) showed significantly restored the decreased levels of brain monoamines such as Noradrenaline, Dopamine & 5-Hydroxy Triptamine. Thus, this study suggests that study of 5-[2-Dimethyl amino ethoxy] Indole 2,3-dione(IIIa) and 5-[2-dimethyl amino ethoxy] Indole 2-one,3-semicarbazone(IVa) increased the monoamines on rat brain, which may be decreased the susceptibility to MES induced seizure in rats.
新的杂环化合物用于治疗癫痫。在本工作中，合成并表征了新的吲哚衍生物，即 5-[2(3)-二烷基氨基烷氧基]吲哚 2,3-二酮衍生物，这些化合物进行了急性毒性试验，然后在白化 Wistar 大鼠上进行了最大电休克（MES）发作模型的抗癫痫活性筛选。在该研究中，5-[2-二甲基氨基乙氧基]吲哚 2,3-二酮和 5-[2-二甲基氨基乙氧基]吲哚 2-酮、3-缩氨基脲（IVa）与苯妥英相比表现出良好的抗癫痫活性和较低的神经毒性。本研究的目的是研究 5-[2-二甲基氨基乙氧基]吲哚 2,3-二酮和 5-[2-二甲基氨基乙氧基]吲哚 2-酮、3-缩氨基脲（IVa）衍生物对最大电休克（MES）方法诱导癫痫发作后大鼠脑中生物胺浓度的影响。我们的研究目的是研究癫痫发作活动与改变单胺类物质（如去甲肾上腺素（NA）、多巴胺（DA）、5-羟色胺（5-HT））之间的关系，在 MES 癫痫模型中大鼠的前脑中。在 MES 模型中，研究 5-[2-二甲基氨基乙氧基]吲哚 2,3-二酮（IIIa）和 5-[2-二甲基氨基乙氧基]吲哚 2-酮、3-缩氨基脲（IVa）（100mg/kg）显著恢复了脑单胺类物质如去甲肾上腺素、多巴胺和 5-羟色胺的降低水平。因此，这项研究表明，研究 5-[2-二甲基氨基乙氧基]吲哚 2,3-二酮（IIIa）和 5-[2-二甲基氨基乙氧基]吲哚 2-酮、3-缩氨基脲（IVa）增加了大鼠脑内的单胺类物质，这可能降低了大鼠对 MES 诱导癫痫发作的易感性。
