| 3α-羟基-16α，17α-亚甲基-5α-孕甾-20-酮类化合物的合成及生物活性研究 |
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| 引用本文： | 何明华,廖清江.3α-羟基-16α，17α-亚甲基-5α-孕甾-20-酮类化合物的合成及生物活性研究[J].中国药物化学杂志,2008,18(2):101-104. |
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| 作者姓名： | 何明华 廖清江 |
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| 作者单位： | 1. 广东医学院药物化学教研室,广东,东莞,523808
2. 中国药科大学药物化学教研室,江苏,南京,210009 |
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| 摘 要： | 目的设计合成含16α，17α-亚甲基的3-羟基5α-孕甾-20-酮类化合物，并研究其神经细胞的保护作用。方法以3β-羟基5α-孕甾-16-烯-20-酮醋酸酯为起始原料经多步反应合成目标化合物；用谷氨酸引起的神经细胞损伤模型研究其保护作用。结果与结论共合成12个目标化合物，其结构经IR、MS、^1H-NMR谱确证，其中5个目标化合物对谷氨酸引起的神经细胞损伤有保护作用。
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| 关 键 词： | 3α-羟基5α-孕甾-20-酮 神经甾体 合成 抗氧化活性 |
| 文章编号： | 1005-0108(2008)02-0101-04 |
| 收稿时间： | 2007-11-26 |
| 修稿时间： | 2007年11月26 |
Synthesis of 3α-hydroxy-16α,17α-methylene 5α-pregnane-20-one derivatives and the evaluation of their bioactivities |
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| HE Ming-hua,LIAO Qing-jiang.Synthesis of 3α-hydroxy-16α,17α-methylene 5α-pregnane-20-one derivatives and the evaluation of their bioactivities[J].Chinese Journal of Medicinal Chemistry,2008,18(2):101-104. |
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| Authors: | HE Ming-hua LIAO Qing-jiang |
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| Institution: | (1.Department of Medicinal Chemistry, School of Pharmacy , Guangdong Medical University,Dongguan 523808,China; 2. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009,China) |
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| Abstract: | Aim To design and synthesize a series of 3α-hydroxy-5α-pregnane–20-one compounds,and to evaluate their bioactivities Methods The target compounds were synthesized from pregnenolone acetate by serial steps. All of them were confirmed by IR , 1H-NMR and MS. Their protective effects on glutamate-induced neurotoxicity model were studied. Results and conclusion Five target compounds of showed protective effects on glutamate-induced neurotoxicity |
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| Keywords: | 3α-hydroxy-5α-pregnane–20-one neurosteriods synthesis antioxidative activity |
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