Chin. J. Org. Chem. ›› 2007, Vol. 27 ›› Issue (07): 870-873. Previous Articles     Next Articles

Reports

(S)-萘普生-1,4-二氢吡啶类化合物的合成与生物活性

胡艾希*,谢艳丽,伍小云,叶姣   

  1. (a湖南大学化学化工学院 长沙 410082)
    (b南方医科大学药学院 广州 510515)
  • 收稿日期:2006-03-27 修回日期:1900-01-01 发布日期:2007-06-30
  • 通讯作者: 胡艾希*

Synthesis and Bioactivity of 1,4-Dihydropyridine Moiety Substituted (S)-Naproxen

HU Ai-Xi*,XIE Yan-Li,WU Xiao-Yun,YE Jiao   

  1. (a College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082)
    (b College of Pharmaceutical Sciences, South Medical University, Guang-zhou 510515)
  • Received:2006-03-27 Revised:1900-01-01 Published:2007-06-30
  • Contact: HU Ai-Xi*

The target compounds were synthesized by the reaction chloromethyl ester of (S)-naproxen with 1,4-dihydropyridine-3,5-dicarboxylic monoester in DMF in the presence of K2CO3, and purified by gradient crystallization or column chromatography on silica gel. The yields of seven new compounds were 21%~73%. The structures of the compounds were confirmed by 1H NMR, IR and MS spectra. The effect of such new compounds on the contrac-tion of aorta smooth muscle was observed on the isolated arotic strips of rabbits, and most of them could re-lax constricting strip induced by phenylephrine.

Key words: synthesis, bioactivity, 1,4-dihydropyridine moiety substituted (S)-naproxen