新型苯并咪唑类化合物的合成及抗柯萨奇B_3病毒活性  

Synthesis of Novel Benzimidazole Derivatives and Their Antivirus Activity against Coxsackie Virus B_3

作　　者：张钟闾[1] 罗先金[1] 修乃云[2] 彭宗根[3] 滕立[3] 

机构地区：[1]上海交通大学化学化工学院,上海200240 [2]上海师范大学生命与环境科学学院,上海200234 [3]中国医学科学院北京协和医学院医药生物技术研究所,北京100050

出　　处：《中国医药工业杂志》2009年第7期488-492,共5页Chinese Journal of Pharmaceuticals

摘　　要：3-硝基邻苯二甲酸酐经氨解、Hoffman降解、水合肼还原及闭环反应得2-芳基-1H-苯并咪唑-4-羧酸,经氯化亚砜酰氯化后与相应的胺反应,制得2-取代芳基-1H-苯并咪唑-4-酰胺类衍生物1a～1g,均为新化合物。并测定了其抑制柯萨奇B3病毒(CVB3)活性。结果显示,化合物1b、1c、1e和1g的活性优于利巴韦林。A series of new benzimidazole derivatives 1a -1g were synthesized from 3-nitrophthalic anhydride by ammonolysis, Hoffman degradation and reduction with hydrazine hydrate to give 2,3-diaminobenzoic acid, which was subjected to cyclization with aldehydes, chlorination with SOCl2, followed by amidation with amines. The test of their activity against Coxsackie virus B3 （CVB3） in Vero cells showed that compounds 1b, 1c, 1e and lg had the better activity than that of ribavirin.

关 键 词：苯并咪唑 柯萨奇B3病毒(CVB3) 抗病毒活性 合成 

分 类 号：O626[理学—有机化学]