系列烟酸前体药物的合成  

Synthesis of a series of nicotinic acid prodrugs

作　　者：熊晓云[1] 邹永[2] 刘毅 招明高[1] 钟裕国[4] 

机构地区：[1]第四军医大学基础部,陕西西安710032 [2]中国科学院广州化学研究所,广东广州510650 [3]陕西省卫生防疫站,陕西西安710054 [4]四川大学华西药学院,四川成都610041

出　　处：《中国药物化学杂志》2002年第2期86-87,91,共3页Chinese Journal of Medicinal Chemistry

基　　金：广东省自然科学基金项目 (0 0 0 94 2 )

摘　　要：目的寻找活性更强、副作用更小的烟酸前体药物。方法以烟酸为起始原料 ,采用酰氯法 ,通过酯键或酰胺键 ,分别与对乙酰氨基酚、香草醛、磺胺甲唑、L 苯丙氨酸甲酯、盐酸普鲁卡因及诺氟沙星等药物相偶联 ,合成了 6个新目标化合物。结果化合物的结构均经红外光谱、核磁共振氢谱、质谱及其元素分析确证。Aim To screen out nicotinic acid prodrugs with better activity and less side effects.Methods By employing the acyl chloride method,6 new title compounds were synthesized from nicotinic acid with paracetamol,vanilla aldehyde, L phenylalanine methyl ester,sulfamethoxazole,procaine hydrochloride,and norfloxacin respectively by the ester bond or amide linkage.Results Their chemical structures were determined by IR, 1H NMR,MS and elemental analysis.Conclusion The acyl chloride method was feasible to the synthesis of nicotinic acid prodrugs.

关 键 词：烟酸 前体药物 合成 

分 类 号：R914.5[医药卫生—药物化学]