Synthesis and antimicrobial activity of 3-octyloxy-8-alkyljatrorrhizine derivatives

Abstract

By introducing octyloxy to C-3 and alkyl groups to C-8 of jatrorrhizine, a series of 3-octyloxy-8-alkyljatrorrhizine derivatives were synthesized and their antimicrobial activities were evaluated in vitro. The results indicated that the derivatives exhibited high antimicrobial activities, especially against Gram-positive bacteria. The 3-octyloxy-8-butyljatrorrhizine displayed the highest antimicrobial activity in all compounds. Their structure–activity relationships were discussed.

Keywords:

• jatrorrhizine
• 3-octyloxy-8-alkyljatrorrhizine derivatives
• antimicrobial activity

Acknowledgements

This work was supported by the National Natural Science Foundation of China (20673084), the Natural Science Foundation Project of CQ CSTC (2008BB5257), and the Key Technologies R&D Program of CQ CSTC (2008AA5021).