» Articles » PMID: 30108926

Design, Synthesis and Bioactivities of Phenithionate Analogues or Derivatives for Anti-schistosomiasis

Overview
Journal Medchemcomm
Specialty Chemistry
Date 2018 Aug 16
PMID 30108926
Citations 1
Authors
Affiliations
Soon will be listed here.
Abstract

A novel series of phenithionate analogues or derivatives were designed and synthesized using phenithionate as the lead compound, and their bioactivities were studied. Their structures were confirmed by H NMR, C NMR, HR-ESI-MS, and elemental analysis, respectively. The results of inhibitory activity measurement proved that compounds , , , , and had a better inhibitory effect on larva and imago schistosoma. Among them, the inhibitory activity of compound for larva schistosoma was IC = 5.21 ± 0.04 μg mL, and for imago schistosoma it was IC = 6.35 ± 0.08 μg mL. Moreover, the experimental results of anti-schistosomiasis activity measurement showed that they had good anti-schistosomiasis activity. Therefore, these compounds had better drugability.

Citing Articles

Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?.

Dziwornu G, Attram H, Gachuhi S, Chibale K RSC Med Chem. 2021; 11(4):455-490.

PMID: 33479649 PMC: 7593896. DOI: 10.1039/d0md00062k.

References
1.
Xiao S, Catto B . In vitro and in vivo studies of the effect of artemether on Schistosoma mansoni. Antimicrob Agents Chemother. 1989; 33(9):1557-62. PMC: 172702. DOI: 10.1128/AAC.33.9.1557. View

2.
Xiao S, Chollet J, Utzinger J, Matile H, Mei J, Tanner M . Artemether administered together with haemin damages schistosomes in vitro. Trans R Soc Trop Med Hyg. 2001; 95(1):67-71. DOI: 10.1016/s0035-9203(01)90336-0. View

3.
Xiao S, Mei J, Jiao P . Further study on mefloquine concerning several aspects in experimental treatment of mice and hamsters infected with Schistosoma japonicum. Parasitol Res. 2009; 106(1):131-8. DOI: 10.1007/s00436-009-1640-5. View

4.
Oliveira M, dAvila J, Tempone A, Correa Soares J, Rumjanek F, Ferreira-Pereira A . Inhibition of heme aggregation by chloroquine reduces Schistosoma mansoni infection. J Infect Dis. 2004; 190(4):843-52. DOI: 10.1086/422759. View

5.
Xiao S, Wu Y, Tanner M, Wu W, Utzinger J, Mei J . Schistosoma japonicum: In vitro effects of artemether combined with haemin depend on cultivation media and appraisal of artemether products appearing in the media. Parasitol Res. 2003; 89(6):459-66. DOI: 10.1007/s00436-002-0786-1. View