| 第 38 卷第 1 期 |  | Vol. 38 No. 1 | | 2008 年 2 月 | Feb 2008 |
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所屬欄目：醫藥及中間體
4-色滿(mǎn)酮芳環(huán)Mannich堿類(lèi)化合物的合成及其抗血小板聚集活性研究 |
| 李慧媛1，張琳琳1，張傳明1，劉曉平1，劉玉蘭1，詹華強2，胡 春1
（1. 沈陽(yáng)藥科大學(xué) 制藥工程學(xué)院，遼寧 沈陽(yáng)110016；2.香港科技大學(xué) 生物系，香港） |
| 摘 要：4-色滿(mǎn)酮類(lèi)化合物和色酮類(lèi)化合物具有廣泛的生物活性。筆者曾發(fā)現4-色滿(mǎn)酮3位Mannich堿類(lèi)化合物具有顯著(zhù)的抗血小板聚集活性，為了考察在4-色滿(mǎn)酮的3-位Mannich堿類(lèi)化合物中3-位胺甲基側鏈是否為加強活性的必需基團，為確定其藥效構象提供信息，筆者設計合成了4種4-色滿(mǎn)酮芳環(huán)Mannich堿類(lèi)化合物，同時(shí)又合成了3種色酮芳環(huán)Mannich堿類(lèi)化合物。所合成的目標化合物均未見(jiàn)文獻報道，其組成和結構經(jīng)紅外光譜、質(zhì)譜和核磁共振氫譜確認。采用Born's比濁法對目標化合物進(jìn)行了抗血小板聚集活性的體外篩選。實(shí)驗結果表明，目標化合物對ADP和膠原誘導的家兔血小板聚集均具有顯著(zhù)的體外抑制活性。 |
| 關(guān)鍵詞：4-色滿(mǎn)酮；色酮；衍生物；合成；抗血小板聚集 |
| 中圖分類(lèi)號：R914 文獻標識碼：A 文章編號：1009-9212（2008）01- 0013-05 |
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| Synthesis and Anti-platelet Aggregative Activity of the Mannich Bases of 4-Chromanones and 4-Chromones |
| LI Hui-yuan1，ZHANG Lin-lin1，ZHANG Chuan-ming1，LIU Xiao-ping1，LIU Yu-lan1，ZHAN Hua-qiang2，HU Chun1
（School of Pharmaceutical Engineering，Shenyang Pharmaceutical University，Shenyang 110016，China；Department of Biology，The Hong Kong University of Science and Technology，Clear Water Bay，Hong Kong，China） |
| Abstract：4-Chromanones and chromones are known to exhibit a wide range of biological activities. Mannich bases at 3-position of 4-chromanones synthesized in our laboratory exhibit the significant anti-platelet aggregative activity. On the base of our previous work，the mannich bases at aromatic ring of 4-chromanones and chromones which were designed as the candidates of platelet aggregative inhibitors were synthesized as shown，the seven target compounds which were not reported in the literature were synthesized and characterized by 1H NMR，IR，LC-MS and GC-MS. The anti-platelet aggregative activity of the target compounds was tested using Born's method. According to screening results，some of the target compounds such as 7-hydroxy-8-（4-morpholinomethyl）-4-chromanone and 7-hydroxy-2，8-di（4-morpholinomethyl）chromone showed potent inhibitory activity against rabbit platelet aggregation induced by ADP in vitro，some of the target compounds such as 7-hydroxy-2，8-di（4-morpholinomethyl）chromone showed potent inhibitory activity against rabbit platelet aggregation induced by collagen in vitro. |
| Key words：4-chromanone；chromones；derivative；synthesis；anti-platelet aggregative |
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基金項目：國家自然科學(xué)基金資助項目（20472053）
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作者簡(jiǎn)介：李慧媛（1977-），女，江蘇徐州人，博士，從事多肽藥物的設計與合成。
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聯(lián) 系 人：胡 春，教授，博士，博士生導師，從事新藥設計與合成研究。（E-mail：chunhu1999@163.com）
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收稿日期：2008-01-25
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