期刊文献+

Synthesis and anti-HIV-1 activity evaluation of N-l-alkyl-5-halogeno-6- alkylamino uracils as novel non-nucleoside HIV-I reverse transcriptase inhibitors

Synthesis and anti-HIV-1 activity evaluation of N-l-alkyl-5-halogeno-6- alkylamino uracils as novel non-nucleoside HIV-I reverse transcriptase inhibitors
原文传递
导出
摘要 N-l-alkyl-5-halogeno-6-alkylamino uracils, which are novel l-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) analogues, were synthesized as the selective and potent non-nucleoside human immunodeficiency virus (HIV)-I reverse transcriptase inhibitors. Some of the compounds showed potent inhibitory activity against HIV-1 reverse transcriptase. For instance, compounds ld, lm and In exhibited potent anti-HIV-1 activity with the ICso values of 13.3, 11.7 and 3.15 μM, respectively, which are comparable to that of nevirapine (IC50 8.38 μM).
出处 《Journal of Chinese Pharmaceutical Sciences》 CAS 2011年第2期146-153,共8页 中国药学(英文版)
基金 Foundation items: National Natural Science Foundation of China (Grant No. 20672008 and 20972011).
  • 相关文献

参考文献19

  • 1Gallo, R.C.; Sarin, RS.; Gelmann, E.E; Robert-Guroff, M.; Richardson, E. Science. 1983, 220, 865-867.
  • 2Barre-Sinoussi, F.; Chermann, J.C.; Rey, F.; Nugeyre, M.T.; Chamaret, S.; Gmest, J.; Dauguet, C.; Axler-Blin, C. Science. 1983, 220, 868-870.
  • 3Essex, M.; Mclane, M.F.; Lee, T.H.; Falk, L.; Howe, C.W.S.; Mullins, J.I. Science. 1983, 220, 859-862.
  • 4Gelmann, E.P.; Popovic, M.; Blayney, D.; Masur, H.; Sidhu, G.; Stahl, R.E.; Gallo, R.C. Science. 1983, 220, 862-865.
  • 5Arnold, E.; Das, K.; Ding, J.; Yadav, EN.S.; Hsiou, Y.; Boyer, P.L.; Hughes, S.H. Drug Des. Discov. 1996, 13, 29-47.
  • 6Gait, M.J.; Karn, J. Trends Biotechnol. 1995, 13, 430-438.
  • 7Giovanni, M.; Marco, R.; Marie-Aline, G.; Maurizio, B.; Eric, E. Viruses. 2010, 2, 880-899.
  • 8Pedersen, O.S.; Pedersen, E.B. Synthesis. 2000, 4, 479-495.
  • 9De Clercq, E. Chem. Biodivers. 2004, 1, 44-64.
  • 10Delaugerre, C.; Rohban, R.; Simon, A. J. Med. Virol. 2001, 65, 445-448.

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