Chin. J. Org. Chem. ›› 2010, Vol. 30 ›› Issue (07): 997-1004. Previous Articles     Next Articles

Full Papers

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

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