Synthesis and antiepileptic studies of new imidazo[1,2-a]pyridine derivatives

来源 :Chinese Chemical Letters | 被引量 : 0次 | 上传用户:keyina
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
In this manuscript,we report the synthesis of newly designed imidazo[1,2-a]pyridines carrying active pharmacophores as potential anticonvulsant agents.Newly synthesized target compounds were characterized by FTIR,1H NMR,13C NMR,and mass spectroscopy followed by elemental analysis studies.Preliminary anticonvulsant screening study of target compounds was carried out following MES and scPTZ methods.Compounds 6e and 6f,possessing electron rich aryl substituent at position-2 and tolyl substituted oxazolone moiety at the position-3 of imidazo[1,2-a]pyridine ring,exhibited activity comparable to standard drug diazepam and emerged as lead compounds.New compounds displayed enhanced activity in scPTZ method,indicating their ability to raise the seizure threshold.Their neurotoxicity study by Rotarod test showed that they are nontoxic at all tested doses. In this manuscript, we report the synthesis of newly designed imidazo [1,2-a] pyridines carrying active pharmacophores as potential anticonvulsant agents. Newly synthesized target compounds were characterized by FTIR, 1H NMR, 13C NMR, and mass spectroscopy followed by elemental analysis studies. Preliminary anticonvulsant screening study of target compounds was carried out following MES and scPTZ methods. Compounds 6e and 6f, possessing electron rich aryl substituent at position-2 and tolyl substituted oxazolone moiety at the position-3 of imidazo [1,2-a ] pyridine ring showed activity comparable to standard drug diazepam and emerged as lead compounds. New compounds displayed enhanced activity in scPTZ method, indicating their ability to raise the seizure threshold. Their neurotoxicity study by Rotarod test showed that they are nontoxic at all tested doses .
其他文献
目的 针对风湿性心瓣膜炎的早期诊断 ,建立一项检测抗心瓣膜蛋白抗体的方法 ,并探讨其临床意义。方法 采用ELISA法检测抗心瓣膜蛋白抗体 (AVP) ,比较 30例风湿性心瓣膜炎、
2012年全球化学品销售额共3.3万亿美元,其中特种化学品规模4980亿美元,占比达15%。未来5年,全球特种化学品市场还将以年均3.7%的速度继续增长。亚洲已成为世界特种化学品最大
Effect of rare earth alloy modification on properties and microstructure of high carbon equivalent gray cast iron was investigated.The experimental results show
通过配体交换的方法成功将含糖聚合物PGAMA14-PCL32-SH接枝到纳米金棒的表面(Gly@AuNRs).借助X-射线光电子能谱(XPS)、动态光散射(DLS)、热重分析(TGA)等对Gly@AuNRs进行了表
综述了用于燃料电池中氧还原反应(ORR)的石墨烯衍生物负载的各种纳米催化剂的最新进展.介绍了用于表征石墨烯基电催化剂的常规电化学技术以及石墨烯基电催化剂最新的研究进展
7月4日,广西田园生化股份有限公司获批临时登记国内企业第2批毒氟磷产品,分别是98%原药和30%可湿性粉剂(登记作物和防治对象为番茄病毒病、水稻黑条矮缩病)。此前,广西田园生
Two novel thieno-[3,4-b]-pyrazine-based molecules,TP-E and TP-O,were designed and synthesized for potential application as red fluorescent emitters.The bulky te
目的:建立喜马拉雅紫茉莉根中胡芦巴碱含量测定的HPLC法,考察海拔和生长年限对药材中胡芦巴碱含量的影响。方法:采用Agilent Porlaris-NH2色谱柱,流动相乙腈-水(87∶13),检测
20世纪90年代以来,世界各国对发动机排放法规的不断严格大大推动了发动机技术的发展。2005年欧洲车用发动机已开始实行欧Ⅳ排放法规,对柴油机提出了更为苛刻的要求。欧洲NOx
近来,我院遇到5例使用氧氟沙星注射液致白细胞减少的高龄患者,现举2例典型病例报告如下。例1:男,88岁。因言语不清、四肢活动不灵6年,门诊以多发性腔隙性脑梗塞、老年性脑萎缩、高血压Ⅲ