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  • Title: Synthesis, characterization and biological evaluation of novel 6-ferrocenyl-4-aryl-2-substituted pyrimidine derivatives.
    Author: Parveen H, Hayat F, Salahuddin A, Azam A.
    Journal: Eur J Med Chem; 2010 Aug; 45(8):3497-503. PubMed ID: 20488588.
    Abstract:
    A new series of 6-ferrocenyl-4-aryl-2-substituted pyrimidines were synthesized and evaluated for in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. Out of 16 compounds 10 compounds have shown IC(50) values in the range of 0.41-1.73 microM and 1.80 microM. Pyrimidine derivatives having thiomethyl group, chloro group and mono-, di-, and trimethoxy substitution, exhibited higher antiamoebic activity than the reference drug metronidazole (IC(50)=1.80 microM). The toxicological studies of these compounds on human kidney epithelial cell line showed that all compounds were non-toxic. 4-(4-Chlorophenyl)-6-ferrocenyl-2-piperidin-1-yl-pyrimidine (4f) was found most active (IC(50)=0.41 microM) and least toxic among all the compounds.
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