Synthesis and Antimicrobial Activity of 8-Alkyl Coptisine Derivatives
Xiao-Fei Jiang
Chemistry Institute of Pharmaceutical Resources, School of Pharmaceutical Science, Southwest University, Chongqing 400716, P.R. China; College of Chemical and Environmental Engineering, Chongqing Three Gorges University, Chongqing 404000, P.R. China
Xiao-Li Ye
School of Life Science, Southwest University, Chongqing 400715, P.R. China
Baoshun Zhang
Chemistry Institute of Pharmaceutical Resources, School of Pharmaceutical Science, Southwest University, Chongqing 400716, P.R. China
Xue-Gang Li
Chemistry Institute of Pharmaceutical Resources, School of Pharmaceutical Science, Southwest University, Chongqing 400716, P.R. China
Xingyan Liu
College of Chemistry and Materials Sciences, Sichuan Normal University, Chengdu 610068, P.R. China
Corresponding Author(s) : Xue-Gang Li
xuegangli2000@yahoo.com.cn
Asian Journal of Chemistry,
Vol. 23 No. 9 (2011): Vol 23 Issue 9
The compounds 8-butyl (2), 8-hexyl- (3), 8-octyl- (4), 8-decyl (5) and 8-dodecylcoptisine chloride (6) were synthesized and their antimicrobial activities were tested in vitro. LD50 were tested by mice's abdominal cavity injection in order to evaluate their structure-activity relationships. The results indicated that the derivatives exhibited high antimicrobial activities than coptisine, especially against Gram-positive bacteria and fungi. The 8-octylcoptisine displayed the highest antimicrobial activity in all compounds. The toxicity of compounds 2-6 was stronger than that of coptisine. However, upon elongating the aliphatic chain, the toxicity decreased gradually.
Jiang, X.-F., Ye, X.-L., Zhang, B., Li, X.-G., & Liu, X. (2011). Synthesis and Antimicrobial Activity of 8-Alkyl Coptisine Derivatives. Asian Journal of Chemistry, 23(9), 3849–3852. Retrieved from https://asianpubs.org/index.php/ajchem/article/view/10748
