CN101033239A - 一个新的类胰岛素药物模型化合物的制备与结构 - Google Patents
一个新的类胰岛素药物模型化合物的制备与结构 Download PDFInfo
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Abstract
钒能促进血糖运输和新陈代谢，生物脂、DNA和蛋白质的合成，也能促进细胞分裂。此外，钒酸盐还有刺激血糖吸收、糖解及抗肿瘤等功能。但由于VO2+有毒性，且不易吸收，本发明是通过选择适当的取代基聚吡唑硼酸盐为配体与钒化合形成四价或五价有机钒化合物来降低毒性。因为它具有很强的配位能力，并且能够控制和稳定钒氧配合物，以达到定向设计、调控分子构型和特性的目的。
Description
技术领域
本项专利涉及到一个新类胰岛素药物模型化合物的制备及其结构表征。此化合物的合成方法简单，条件易控制，原料易得。
技术背景
目前，人们对医治糖尿病类药物分子的设计与合成的研究越来越重视，尤其是类胰岛素药物的开发与研制。其中，相关类胰岛素活性钒类化合物的研究倍受关注。因为，虽然钒在植物和动物体内含量极少，但它的化合物却具有非常有趣的生物和药物活性，尤其是类胰岛素活性。钒能促进血糖运输和新陈代谢，生物脂、DNA和蛋白质的合成，也能促进细胞分裂。此外，钒酸盐还有刺激血糖吸收、糖解及抗肿瘤等功能。总之，研究钒的金属-有机配体化合物的结构、特性及生物活性的关系，对深入了解这些金属药物与体内生物大分子作用，治疗糖尿病疾病的机制及其药理作用具有重要意义。但由于VO2+有毒性，且不易吸收，因此科学家们把精力集中在延长药物作用时间和降低药物的毒性上。本发明是通过选择适当的取代基聚吡唑硼酸盐为配体与钒化合形成四价或五价有机钒化合物来降低毒性。因为它具有很强的配位能力，并且能够控制和稳定钒氧配合物，以达到定向设计、调控分子构型和特性的目的。
发明内容
聚吡唑硼酸盐与VOSO4·nH2O和吡咯啶二硫代氨基甲酸铵在溶剂中混合，搅拌，在常温下析出一种新型的具有潜在的胰岛素功能模拟药物作用的钒聚吡唑硼酸盐配合物。反应机理如下：
所选溶剂有：甲醇，乙醇，四氢呋喃，N，N-二甲基甲酰胺等。
反应温度为25-60℃，且不宜超过60℃。
配合物表征仪器：C，H，N分析用PE 240C型分析仪测定；红外光谱用JASCOFT/IR-480型光谱仪测试(4000-200cm-1)；紫外光谱用JASCO V-570型光谱仪测试(200-1100nm)；晶体结构数据用X-射线衍射分析(APEX II CCD型衍射仪)测试。
结构表征：红外光谱分析见图1，主要峰归属如下：νB-H 2478cm-1，νV＝O 967cm-1，νC-S1050cm-1，νV-S 372cm-1。紫外光谱见图2，主要峰归属如下：LMCT：232nm。分子结构见图3。热稳定性测试结果见图4，分析结果如下：此化合物分三步分解，分解温度分别为：261，450，571℃。
附图说明
图1为红外光谱。
图2为紫外光谱。
图3为VO(HB(pz)3)(C5H8NS2)的结构图。
图4为热稳定性测试结果。
具体实施方式
实例1
将0.238g(1mmol)NaHB(pz)3溶于5ml甲醇中；将0.199g，(1mmol)VOSO4·nH2O和0.164g(1mmol)吡咯啶二硫代氨基甲酸铵溶于5ml甲醇中。将上述两种溶液混合，搅拌6h，得到黄绿色溶液，并逐渐有黄绿色沉淀出现。然后，过滤，沉淀用甲醇洗涤，在空气中干燥，得到蓝色固体和黄绿色溶液。固体化合物重0.30g，产率为70％，将固体化合物在CH2Cl2/MeOH(5∶2)中重结晶，几天后得到适合于X-射线衍射分析的蓝色晶体。元素分析：理论值，C 39.42，H 4.22，N 22.99％；实测值，C 39.25，H 4.55，N 22.46％。
实例2
将0.238g(1mmol)NaHB(pz)3溶于5ml乙醇中；将0.199g，(1mmol)VOSO4·nH2O和0.164g(1mmol)吡咯啶二硫代氨基甲酸铵溶于5ml乙醇中。将上述两种溶液混合，搅拌6h，得到黄绿色溶液，并逐渐有黄绿色沉淀出现。然后，过滤，沉淀用乙醇洗涤，在空气中干燥，得到蓝色固体和黄绿色溶液。固体化合物重0.28g，产率为65％，将固体化合物在CH2Cl2/EtOH(5∶2)中重结晶，几天后得到适合于X-射线衍射分析的蓝色晶体。元素分析：理论值，C 39.42，H 4.22，N 22.99％；实测值，C 39.25，H 4.55，N 22.46％。
Claims (4)
1.一种合成含有聚吡唑硼酸盐和吡咯啶二硫代氨基混合配体的钒氧配合物的制备方法，其特征在于合适的溶剂中进行，在25-60℃、常压条件下进行。
2.按照权利要求1所述，其特征是提纯产品的方法。
3.按照权利要求1所述，其中选择甲醇溶剂最好。
4.按照权利要求1所述，其特征是在温度不宜超过60℃。
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101953846A (zh) * | 2010-06-24 | 2011-01-26 | 攀枝花兴辰钒钛有限公司 | 一种药物组合物在制备治疗糖尿病的药物中的用途 |
| CN101972273A (zh) * | 2010-10-29 | 2011-02-16 | 攀枝花兴辰钒钛有限公司 | 一种药物在制备治疗糖尿病的药物中的用途 |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101953846A (zh) * | 2010-06-24 | 2011-01-26 | 攀枝花兴辰钒钛有限公司 | 一种药物组合物在制备治疗糖尿病的药物中的用途 |
| CN101978965A (zh) * | 2010-06-24 | 2011-02-23 | 攀枝花兴辰钒钛有限公司 | 一种药物在治疗糖尿病中的用途 |
| CN101953846B (zh) * | 2010-06-24 | 2011-12-28 | 攀枝花兴辰钒钛有限公司 | 一种药物组合物在制备治疗糖尿病的药物中的用途 |
| CN101978965B (zh) * | 2010-06-24 | 2011-12-28 | 攀枝花兴辰钒钛有限公司 | 一种药物在治疗糖尿病中的用途 |
| CN101972273A (zh) * | 2010-10-29 | 2011-02-16 | 攀枝花兴辰钒钛有限公司 | 一种药物在制备治疗糖尿病的药物中的用途 |
| CN101972273B (zh) * | 2010-10-29 | 2011-12-21 | 攀枝花兴辰钒钛有限公司 | 一种药物在制备治疗糖尿病的药物中的用途 |
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