Synthesis of hexahydro-1H-1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiary amide) ethane and their analgesic effects
文献类型：期刊论文
| 作者 | Shen, JS ; Lei, LJ; Li, JF; Ji, RY
|
| 刊名 | CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
 |
| 出版日期 | 2002-04 |
| 卷号 | 23期号:4页码:585-590 |
| 关键词 | selective kappa-opioid receptor agonists analgesic effect hexahydro-1H-1 4-diazepine analogues (1-arylacetamide-2-tertiary amide) ethane structure |
| ISSN号 | 0251-0790 |
| 文献子类 | Article |
| 英文摘要 | In order to get some selective kappa-opioid receptor agonists, which can relieve pain while lacking serious side effects, 16 target compounds of hexahydro-H-1-1, 4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiary amide) ethane were synthesized through single amidation and amidation of the basic modified structures of compounds 1-3, 2- (5-) substituted hexahydro-H-1-1, 4-diazepine. The structures of these products were characterized by IR, EIMS, elementary analysis and H-1 NMR. All the target compounds were screened in vitro in the guinea pig ileum(GPI) for their receptor affinities. The preliminary pharmacology tests indicated that these compounds showed a certain agonist activity (presented in the item of inhibition rate) respectively at 5 X 10(-6)mol/L level and the IC50 values(mumol/L) of compounds 5, 7 were achieved. The antinociceptive potencies of the compounds with a higher potency (compounds 5, 13, 22, 23) in the GPI study were further tested their in the mouse abdominal constriction model and their ED50 values (mg/kg, s. c.) were also obtained. |
| WOS关键词 | FUNCTIONAL EXPRESSION ; OPIOID RECEPTOR ; CLONING |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:990649 |
| WOS记录号 | WOS:000175203800018 |
| 出版者 | HIGHER EDUCATION PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274370]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Ji, RY |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Shen, JS,Lei, LJ,Li, JF,et al. Synthesis of hexahydro-1H-1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiary amide) ethane and their analgesic effects[J]. CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,2002,23(4):585-590. |
| APA | Shen, JS,Lei, LJ,Li, JF,&Ji, RY.(2002).Synthesis of hexahydro-1H-1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiary amide) ethane and their analgesic effects.CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,23(4),585-590. |
| MLA | Shen, JS,et al."Synthesis of hexahydro-1H-1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiary amide) ethane and their analgesic effects".CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE 23.4(2002):585-590. |
入库方式： OAI收割
来源：上海药物研究所
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