Synthesis and Bioactivity of Arecoline Derivatives Containing Amino-s-triazole Coupled Oxadiazole  

作　　者：Guo Qiang HU Sheng LI Wen Long HUANG Hai WANG 

机构地区：[1]Medical College of Henan Unversity, Kaifeng 475001 [2]China Pharmaceutical University, Nanjing 210009 [3]Academy of Military Medical Sciences, Beijing 100850

出　　处：《Chinese Chemical Letters》2006年第1期19-22,共4页中国化学快报（英文版）

基　　金：supported by the State Basic Research and Development Project(No.G 1998051112);the Science Foundation of Henan University(04ZDZR009).

摘　　要：5-（5＂-Substituted phenyl-[1＂,3＂,4＂]oxadiazol-2＂-yl methylsulfanyl）-3-pyridin-3′-yl- [1,2,4] triazol-4-yl amines la-j were quaternarized with methyl iodide to afford the corresponding methyl pyridinium salts 2a-j. The reduction of compounds 2 with NaBH4 in methanol gave the target compounds 5-（5＂-substituted phenyl-[1＂,3＂,4＂]oxadiazol-2＂-yl methylsulfanyl）-3-（1′-methyl-1＇,2＇,5＇,6＇-tetrahydropyridin-3＇-yl）-[1,2,4]triazol-4-ylamines 3a-j. The endothelium vascular relaxing activity of the target compounds were screened.5-（5＂-Substituted phenyl-[1＂,3＂,4＂]oxadiazol-2＂-yl methylsulfanyl）-3-pyridin-3′-yl- [1,2,4] triazol-4-yl amines la-j were quaternarized with methyl iodide to afford the corresponding methyl pyridinium salts 2a-j. The reduction of compounds 2 with NaBH4 in methanol gave the target compounds 5-（5＂-substituted phenyl-[1＂,3＂,4＂]oxadiazol-2＂-yl methylsulfanyl）-3-（1′-methyl-1＇,2＇,5＇,6＇-tetrahydropyridin-3＇-yl）-[1,2,4]triazol-4-ylamines 3a-j. The endothelium vascular relaxing activity of the target compounds were screened.

关 键 词：TETRAHYDROPYRIDINE triazolylamine OXADIAZOLE muscarinic agonist vascular activity. 

分 类 号：O626[理学—有机化学] R972[理学—化学]