Vol. 5, Issue 5 (2017)
Structural modification of dihydroartemisinin and antimicrobial assessment of the deoxy and disulphide derivatives
Author(s): Etim EI, Attih EE and Owaba DAC
Abstract:
Dihydroartemisinin is the active metabolite of all artemisinin compounds and is active against all human malaria parasites including multi-drug resistant Plasmodium falciparum strains. Isosteric structural modification of dihydroartemisinin was done by replacing the peroxide bond with disulphide, assessing the characteristics of the products formed and the in vivo antiplasmodial efficacy using mice was confirmed. The present study was aimed at assessing the in vitro antimicrobial potency or otherwise of the deoxy and disulfide derivatives of dihydroartemisinin. Pure dihydroartemisinin solution was chemically reduced using hydrogen generated in situ from zine pellet and dilute hydrochloric acid. Chloroform was used to extract the organic phase. The reduced product was dissolved in dimethylsulphoxide and oxidized using hydrogen sulphide gas. The presence of sulfur in the synthesized compounds was confirmed using standard tests. GC-MS properties of the original starting material dihydroartemisinin, the deoxy and disulphide derivatives were analyzed. The in vitro antimicrobial test of the synthesized drugs using agar diffusion method by pour plate showed activity against Pseudomonas aeruginosa and Aspergllus niger for deoxyartemisinin while, disulfide derivative showed activity against Escherichia coli, Pseudomonas aeruginosa and Aspergillus niger. The minimal Inhibitory Concentrations of the drugs against the susceptible organisms were also established. The synthesized drugs inhibited the microbial growth of Gram negative organisms (Pseudomonas aeruginosa and Escherichia coli) and Aspergillus niger (a fungus), indicating their potential as antimicrobial agents against gram negative organisms and some fungi species.
Pages: 2079-2083 | 776 Views 62 Downloads
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How to cite this article:
Etim EI, Attih EE, Owaba DAC. Structural modification of dihydroartemisinin and antimicrobial assessment of the deoxy and disulphide derivatives. Int J Chem Stud 2017;5(5):2079-2083.
