2,4-dimethoxyphenylsemicarbazones with anticonvulsant activity against three animal models of seizures: Synthesis and pharmacological evaluation

被引：76

作者：

Thirumurugan, R

Sriram, D

Saxena, A

Stables, J

Yogeeswari, P ^{[1
]}

机构：

[1] Birla Inst Technol & Sci, Med Chem Res Lab, Pharm Grp, Pilani 333031, Rajasthan, India

[2] Natl Inst Hlth, Preclin Pharmacol Sect, Epilepsy Branch, Bethesda, MD 20892 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 09期

关键词：

aryl semicarbazones; anticonvulsant; 2,4-dimethoxy; GABA;

D O I：

10.1016/j.bmc.2005.12.041

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Various 2.4-dimethoxyphenylsemicarbazones were synthesized starting from 2,4-dimethoxyaniline via a phenylcarbamate intermediate. The structures were confirmed by spectral and elemental analyses. The anticonvulsant activity of the synthesized compounds was established after intraperitoneal administration in three seizure models in mice which include maximal electroshock seizure, Subcutaneous pentylenetetrazole, and subcutaneous strychnine-induced seizure screens. Nine Compounds exhibited protection in all the three seizure models, and N-1-(2,4-dimethoxyphenyl)-N-4-(propan-2-one)semicarbazone (17) emerged as the most active compound with no neurotoxicity. These compounds were found to elevate gamma-aminobutyric acid (GABA) levels in the midbrain and medulla oblongata regions equipotent to clobazam. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3106 / 3112

页数：7

共 26 条

[21] Synthesis of aryl semicarbazones as potential anticonvulsant agents [J].