Citation: Guo Qiang HU, Sheng LI, Wen Long HUANG, Hai WANG. Synthesis and Bioactivity of Arecoline Derivatives Containing Amino-s-triazole Coupled Oxadiazole[J]. Chinese Chemical Letters, ;2006, 17(1): 19-22. shu

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

1.
Medical College of Henan Unversity, Kaifeng 475001;
2.
China Pharmaceutical University, Nanjing 210009;
3.
Academy of Military Medical Sciences, Beijing 100850

Received Date: 20 May 2005

Fund Project: This project was supported by the State Basic Research and Development Project (No. G 1998051112) and the Science Foundation of Henan University (04ZDZR009).

5-(5"-Substituted phenyl-[1", 3", 4"]oxadiazol-2"-yl methylsulfanyl)-3-pyridin-3'-yl-[1,2,4] triazol-4-yl amines 1a-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.
- Tetrahydropyridine,
- triazolylamine,
- oxadiazole,
- muscarinic agonist,
- vascular activity
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