4.5 Article

Synthesis, Characterization, and Anti-Amoebic Activity of N-(Pyrimidin-2yl) benzenesulfonamide Derivatives

期刊

CHEMISTRY & BIODIVERSITY
卷 10, 期 12, 页码 2267-2277

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.201300009

关键词

Sulfonamides; Pyrimidin-2-amine; Chalcones; Anti-amoebic activity; Structure-activity relationship (SAR)

资金

  1. UGC MANF [F. 40-65(C/M)/2009(SA-III/MANF)]

向作者/读者索取更多资源

A new series of N-(pyrimidin-2-yl)benzenesulfonamide derivatives, 3a-3i and 4a-4i, was synthesized from pyrimidin-2-amines, 2a-2i, with the aim to explore their effects on in vitro growth of Entamoeba histolytica. The chemical structures of the compounds were elucidated by elemental analysis, FT-IR, H-1- and C-13-NMR, and ESI mass-spectral data. In vitro anti-amoebic activity was evaluated against HM1:IMSS strain of Entamoeba histolytica. The IC50 values were calculated by using the double dilution method. The results were compared with the IC50 value of the standard drug metronidazole'. The selected compounds were tested for their cytotoxic activities by cell-viability assay using H9C2 cardiac myoblasts cell line, and the results indicated that all the compounds displayed remarkable >80% viabilities to a concentration of 100 mu g/ml.

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