In Silico Screening of Antimalarial From Indonesian Medicinal Plants Database to Plasmepsin Target

Rifai, Eko Aditya; Hayun, Hayun; Yanuar, Arry

doi:10.22159/ajpcr.2017.v10s5.23115

Cited by 1 publication

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“…Continuing the work of earlier studies attempting to identify new and potent antimalarial treatments [14][15][16][17][18][19][20], in this study, we synthesized modified structures of triclosan and evaluated their antimalarial activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, and in Vitro Antimalarial Activity of Dihydroxylation Derivatives of Triclosan

Fitriana

Yanuar²,

Arsianti³

et al. 2020

Int J App Pharm

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Objective: The emergence of malaria as a global health problem over the past few decades, accompanied by the rise of chemoresistant strains ofPlasmodium falciparum, has emphasized the need for the discovery of new therapeutic drugs against this disease. In this study, enantiomericallyenriched (enantioenriched) analogs of triclosan were synthesized and evaluated for antimalarial activity against P. falciparum cultures.Methods: Enantioselective dihydroxylation of the olefin in amide seven was performed efficiently using chiral quinine ligand (DHQ)2PHAL to yieldenantioenriched dihydroxy propionamide derivative (+)-1 in moderate yields. In a similar way, the chiral quinidine ligand (DHQD)2PHAL was used asstereoselectivity agent yielded the desired enantioenriched (−)-1. The enantioenriched products were used for further in vitro assay, and accordingly thepercent enantiomeric excess (% ee) was not determined. The structures of compounds were proven by spectral data (1H NMR, 13C NMR, and mass spectra).Results: The phenol moiety at the C1 position of triclosan was chemically substituted with a methoxy group, in conjunction with an introducedstereocenter in a 2,3-dihydroxy-propionamide group at C2’ position. Unmodified triclosan inhibited the P. falciparum cultures with an IC50 value of27.2 μM. By contrast, the triclosan analogs, compounds (+)-1 and (−)-1, inhibited the P. falciparum cultures with IC50 values of 0.034 and 0.028 μM,respectively.Conclusion: Collectively, our preliminary in vitro results suggest that these triclosan analogs have potent antimalarial activity and represent apromising new treatment strategy on further development.

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