期刊文献+

Synthesis, Crystal Structure and Biological Activities of Naproxen-eugenol Ester Prodrug

Synthesis, Crystal Structure and Biological Activities of Naproxen-eugenol Ester Prodrug
原文传递
导出
摘要 The prodrug, naproxen-eugenol ester, was synthesized by acyl chloride method with naproxen and eugenol as the raw materials. The structure was identified by proton nuclear magnetic resonance(~H NMR), mass spectrometry(MS), infrared spectrometry(IR) and X-ray diffraction. The compound was crystallized in the or- thorhombic system, space group P21212t with unit cell dimensions a=0.60563(12) nm, b=1.0234(2) nm, c=3.2654(7) nm, a=90°, β=90°, γ=90°, V=2.0240(7) nm3, Z=4. Calculated density 1.235 Mg/m3; absorption coefficient: 0.083 mm-1; F(000)=800; final R1=0.0564. The analgesic activity and anti-inflammatory were similar to those of naproxen, and the results of ulcerogenic activity indicate that the prodrug can significantly decrease the irritation after oral ad- ministration. The prodrug, naproxen-eugenol ester, was synthesized by acyl chloride method with naproxen and eugenol as the raw materials. The structure was identified by proton nuclear magnetic resonance(~H NMR), mass spectrometry(MS), infrared spectrometry(IR) and X-ray diffraction. The compound was crystallized in the or- thorhombic system, space group P21212t with unit cell dimensions a=0.60563(12) nm, b=1.0234(2) nm, c=3.2654(7) nm, a=90°, β=90°, γ=90°, V=2.0240(7) nm3, Z=4. Calculated density 1.235 Mg/m3; absorption coefficient: 0.083 mm-1; F(000)=800; final R1=0.0564. The analgesic activity and anti-inflammatory were similar to those of naproxen, and the results of ulcerogenic activity indicate that the prodrug can significantly decrease the irritation after oral ad- ministration.
出处 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2013年第2期245-248,共4页 高等学校化学研究(英文版)
关键词 Naproxen-eugenol ester Crystal structure Biological activity Naproxen-eugenol ester Crystal structure Biological activity
  • 相关文献

参考文献16

  • 1Pan H., Strait Pharmaceutical Journal, 2005, 17(2), 105.
  • 2Zhao J. F., Chinese Journal of Clinical Rational Drug Use, 2011, 4(6),159.
  • 3Shanbhag V R., Crider A. M., Gokhale R., Harpalani A, Dick R. M., J Pharm. Sci., 1992,81(2), 149.
  • 4Lau W. M., White A w., Gallagher S. J., Donaldson M., McNaughton G., Heard C. M., Curr. Pharm. Des., 2008, 14(8), 794.
  • 5Huang Z. J., Velazquez C. A, Abdellatif K. R. A, Chowdhur M. A, Reisz I. A, DuMond I. F., King S. B., Knaus E. E., J Med. Chem., 2011,54(5), 1356.
  • 6Bonina F. P, Puglia c., Barbuzzi T, Caprariis P., Palagiano F., Rimoli M. G., SaijaA, Eur. J. Pharm. Sci., 2001,14(2),123.
  • 7Sheha M., Khedr A., Elsherief H., Eur. J Pharm. Sci., 2002, 17(3), 121.
  • 8Yan T, Yu G. P, Liu P F., Xiong L. X., Yu S 1., Li Z M., Chem. Res. Chinese Universities, 2012, 28(1), 53.
  • 9Li H. X., Chen X. T, Xu L. Z., Chem. Res. Chinese Universities, 2011, 27(3), 431.
  • 10Sun Y, Huang D. W., Li X. H., Hu J. E., Xiu Z. L., Chem. Res. Chinese Universities, 2012, 28(1),108.

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部