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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (07): 997-1004. 上一篇    下一篇

研究论文

新型二氢吡啶类钙拮抗剂化合物的合成与生物活性

陈国华*1，王丽1，姚秀梅1，张明亮1，吴斐华2   

  1. (1中国药科大学药物化学教研室 南京 210009)
    (2中国药科大学中药药理教研室 南京 210009)
  • 收稿日期:2009-09-15 修回日期:2009-12-11 发布日期:2010-02-01
  • 通讯作者: 陈国华1 E-mail:cgh63@163.com

Synthesis and Biological Activity of Dihydropyridine Calcium Antagonists

Chen Guohua*1 Wang Li1 Yao Xiumei1 Zhang Mingliang1 Wu Feihua2   

  1. (1Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009) (2Department of Pharmacology for Chinese Materia Medica, China Pharmaceutical University, Nanjing 210009)
  • Received:2009-09-15 Revised:2009-12-11 Published:2010-02-01

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1605

被引次数

16 | 4

以1,4-二氢-2,6-二甲基-4-(3-硝基苯基)-3,5-吡啶二羧酸单甲酯()或双乙烯酮为原料, 设计合成了16个未见文献报道的二氢吡啶类钙拮抗剂化合物～及～, 利用IR, H NMR, ESI-MS和元素分析对目标化合物的结构进行表征. 离体大鼠胸主动脉血管环收缩实验表明, 化合物, ～对KCl所致的血管环收缩有明显的舒张作用, 其生物活性均强于阳性对照苯磺酸左旋氨氯地平.

关键词: 二氢吡啶类钙拮抗剂, 合成, 生物活性

Sixteen new dihydropyridine calcium antagonists  and  were designed and synthesized based on 5-(methoxycarbonyl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid ()or diketene. The structures of the target compounds were confirmed byIR,H NMR, ESI-MS techniques and elemental analysis. The results of preliminary pharmacological test showed that compounds , ,, and had obvious relaxation effect on the contraction of vascular ring of aorta induced by KCl, which were better than positive control (levoamlodipine besylate).

Key words: dihydropyridine calcium antagonist, synthesis, biological activity