引用本文:
杨锐生, 胡国强, 张忠泉, 黄文龙. 含噻二唑硫醚的槟榔碱新衍生物的合成及舒张血管活性[J]. 应用化学,
2007, 24(5): 499-502.
Citation: YANG Rui-Sheng, HU Guo-Qiang, ZHANG Zhong-Quan, HUANG Wen-Long. Synthesis and Vascular Relaxing Activity of New Arecoline Analogues Containing Thiadiazole Sulfanylether[J]. Chinese Journal of Applied Chemistry, 2007, 24(5): 499-502.
Citation: YANG Rui-Sheng, HU Guo-Qiang, ZHANG Zhong-Quan, HUANG Wen-Long. Synthesis and Vascular Relaxing Activity of New Arecoline Analogues Containing Thiadiazole Sulfanylether[J]. Chinese Journal of Applied Chemistry, 2007, 24(5): 499-502.
含噻二唑硫醚的槟榔碱新衍生物的合成及舒张血管活性
English
Synthesis and Vascular Relaxing Activity of New Arecoline Analogues Containing Thiadiazole Sulfanylether
Abstract:
The title compounds were designed and synthesized by condensation of the intermediate of pyridinylthiadiazolyl-thiol 3 with various halides to pyridyl-substituted thiadiazole sulfanylethers (4a~4e),followed by the quaternization of compounds 4a~4e with methyl iodide to afford the corresponding methylpyridiniun salts (5a~5e),and reduction of compounds 5a~e with sodium borohydride to give a series of the corresponding target compounds 6a~6e containing the thiadiazole sulfanylether moiety at the 3-position of tetrahydropyridine ring.The structures of the synthesized compounds were characterized by IR,1H NMR,MS spectra and element analysis.The in vitro vascular relaxing activity of target compounds 6a~6e were screened at the concentration 10 μmol/L,their vascular relaxing effects on isolated endothelial cells are 22%,32%,40%,46% and 8%,respectively,while arecoline as reference drug was 21% at the same conditions.
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Key words:
- arecoline derivative
- / tetrahydropyridine
- / thiadiazole
- / synthesis
- / vascular relaxing activity
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