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Synthesis and anticonvulsant activity of some 1,4-dihydropyridine derivatives
Indian Journal of Chemistry, Section B ( IF 0.456 ) Pub Date : 2021-03-03
Safia Begum, Kalam Sirisha

A series of asymmetrical 4-alkyl/aryl-2,6-dimethyl-3-N-(aryl/heteroaryl)-carbamoyl-5-ethoxycarbonyl-1, 4-dihydropyridines 3a-d and symmetrical 4-alkyl/aryl-2,6-dimethyl-3,5-bis-(ethoxycarbonyl)-1,4-dihydropyridines 4a and 4b have been prepared by the condensation of various benzaldehydes, ethylacetoacetate, 2-aminopyridine or p-toludine in ethanol (Hantzch method). The structures of all the synthesized 1,4-dihydropyridine derivatives have been confirmed by spectral data (IR, 1H NMR) and elemental analysis. Compounds 3a-c, 4a and 4b (10 mg/kg) have been evaluated for their anticonvulsant effect against pentylenetetrazole- induced convulsions with phenytoin (4 mg/kg) as the standard. The anticonvulsant potential of the newly synthesized compounds have been assessed on the basis of increase in latency (onset time) to induce convulsions; decrease in number of convulsions and increase in latency of death compared to control and standard.

中文翻译:

1,4-二氢吡啶衍生物的合成及其抗惊厥活性

一系列不对称的4-烷基/芳基-2,6-二甲基-3-N-(芳基/杂芳基)-氨基甲酰基-5-乙氧基羰基-1、4-二氢吡啶3a-d和对称的4-烷基/芳基-2, 6-二甲基-3,5-双-(乙氧羰基)-1,4-二氢吡啶4a4b是通过将各种苯甲醛,乙酰乙酸乙酯,2-氨基吡啶或甲苯胺在乙醇中缩合制备的(Hantzch方法)。所有合成的1,4-二氢吡啶衍生物的结构已通过光谱数据(IR,1 H NMR)和元素分析得到证实。化合物3a-c4a4b以苯妥英(4 mg / kg)为标准,已评估(10 mg / kg)对戊戊四唑诱导的惊厥的抗惊厥作用。新合成化合物的抗惊厥潜能已根据诱发惊厥的潜伏期(发作时间)的增加进行了评估。与对照组和标准组相比,惊厥次数减少,死亡潜伏期延长。
更新日期:2021-03-03
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