Synthesis of Derivatives of Artesunate α-Aminophosphonate and Their Antimicrobial Activities
Thirteen α-aminophosphonate derivatives with artesunate were synthesized by introducing
bioactive α-aminophosphonate combination with artesunate in this work. The reaction were easily carried
out at normal pressure, low temperature and without any catalyst. Four strains of microbials,
namely Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans,
were used for the evaluation of the antimicrobial activities of these target compounds. Experimental results indicated that
most of the compounds had good inhibitory effects. Compound 7k showed obvious antimicrobial activities with the MICs
of 64 μg/ml against Staphylococcus aureus and 32 μg/ml against Candida albicans. Furthermore, when combined with
roxithromycin, the synthesized compounds showed overlapping enhanced activities and proved potential antimicrobial
synergists of roxithromycin.
Keywords: Artesunate, α-aminophosphonate, Antimicrobial Activity, Synthesis.
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