Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Eur J Med Chem. 2010 Aug;45(8):3497-503. doi: 10.1016/j.ejmech.2010.04.023. Epub 2010 Apr 28.
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.
合成了一系列新的 6-二茂铁基-4-芳基-2-取代嘧啶，并对其进行了体外抗溶组织内阿米巴活性评估，以 HM1:IMSS 株溶组织内阿米巴为实验对象。在 16 种化合物中，有 10 种化合物的 IC50 值在 0.41-1.73 μM 和 1.80 μM 范围内。具有硫甲基、氯取代基以及单、二和三甲氧基取代基的嘧啶衍生物表现出比参考药物甲硝唑（IC50=1.80 μM）更高的抗阿米巴活性。这些化合物对人肾上皮细胞系的毒理学研究表明，所有化合物均无毒性。在所有化合物中，4-(4-氯苯基)-6-二茂铁基-2-哌啶-1-基嘧啶（4f）的活性最高（IC50=0.41 μM），毒性最低。
