| 1,5-二取代吡唑-3-甲酰胺类新化合物的合成及其生物活性 |
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| 引用本文： | 代现平,李行舟,郑志兵,李松. 1,5-二取代吡唑-3-甲酰胺类新化合物的合成及其生物活性[J]. 中国药物化学杂志, 2006, 16(6): 331-335 |
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| 作者姓名： | 代现平 李行舟 郑志兵 李松 |
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| 作者单位： | 1. 沈阳药科大学,制药工程学院,辽宁,沈阳,110016
2. 军事医学科学院,毒物药物研究所,北京,100850 |
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| 基金项目： | 国家重点基础研究发展计划(973计划) |
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| 摘 要： | 目的 设计合成新型1,5-二取代吡唑-3-甲酰胺类化合物,并对其抗ALK5活性进行初步评价.方法 以取代的苯乙酮及草酸二甲酯为原料,经多步反应合成目标化合物,用化学发光法检测报告基因表达产物萤火虫萤光素酶活性,计算化合物对ALK5的抑制率.结果与结论 共合成15个未见文献报道的新化合物,其结构经IR、1H-NMR和MS确证.初步生物活性评价结果显示化合物4g具有一定的抗ALK5活性.
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| 关 键 词： | 药物化学:化合物制备 化学合成 1,5-二取代吡唑-3-甲酰胺 ALK5抑制剂 |
| 文章编号： | 1005-0108（2006）06-0331-05 |
| 收稿时间： | 2006-05-08 |
| 修稿时间： | 2006-05-08 |
Synthesis of novel 1, 5-diarylpyrazole-3-carboxamide derivatives and their biological activities |
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| DAI Xian-ping,LI Xing-zhou,ZHENG Zhi-bing,LI Song. Synthesis of novel 1, 5-diarylpyrazole-3-carboxamide derivatives and their biological activities[J]. Chinese Journal of Medicinal Chemistry, 2006, 16(6): 331-335 |
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| Authors: | DAI Xian-ping LI Xing-zhou ZHENG Zhi-bing LI Song |
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| Affiliation: | 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China ; 2. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China |
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| Abstract: | Aim To design and synthesize novel 1,5-diarylpyrazole-3-carboxamide derivatives,and to assay their activities of inhibiting ALK5.Methods The target compounds were synthesized from substituted acetophenone and dimethyl oxalate and the activities of inhibiting ALK5 were assayed by luciferase reporter system transfected in 293 cells.Results and conclusion Fifteen new compounds were synthesized and their structures were confirmed by IR,()~1H-NMR and MS.The primary biological tests showed that compound 4g exhibited some ALK5 inhibitory activity. |
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| Keywords: | medicinal chemistry compound preparation chemical synthesis 1 5-diarylpyrazole-3-carboxamide ALK5 inhibitor |
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