Budakoti Asha, Abid Mohammad, Azam Amir
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Eur J Med Chem. 2007 Apr;42(4):544-51. doi: 10.1016/j.ejmech.2006.10.011. Epub 2006 Dec 6.
Reaction of neutral NS bidentate ligands, 1-N-substituted thiocarbamoyl-3,5-diphenyl-2-pyrazolines, isolated by cyclization of chalcone with N-4-substituted thiosemicarbazide of aromatic amines (1-8), with [Pd(DMSO)(2)Cl(2)] (DMSO=dimethylsulfoxide) leads to the formation of new complexes of the type [Pd(L)Cl(2)] (1a-8a). The structures of the compounds were elucidated by UV, IR, (1)H NMR, (13)C NMR and ESI-MS spectral data and thermogravimetric analysis and their purities were confirmed by elemental analyses. The antiamoebic activity of these complexes was evaluated by microdilution method against HM1:IMSS strain of Entameoba histolytica and the results were compared with the standard drug, metronidazole. Generally palladium complexes showed better activity than their corresponding ligands. Compound 3a showed better IC(50)=0.05 microM as compared to metronidazole IC(50)=1.82 microM.
通过查尔酮与芳香胺的 N-4-取代硫代氨基脲(1-8)环化反应分离得到的中性 NS 双齿配体 1-N-取代硫代甲酰基-3,5-二苯基-2-吡唑啉,与 [Pd(DMSO)₂Cl₂](DMSO = 二甲基亚砜)反应生成新型配合物 [Pd(L)Cl₂](1a - 8a)。通过紫外、红外、¹H NMR、¹³C NMR 和 ESI-MS 光谱数据以及热重分析对化合物结构进行了阐明,并通过元素分析确认了它们的纯度。采用微量稀释法对这些配合物针对溶组织内阿米巴 HM1:IMSS 菌株的抗阿米巴活性进行了评估,并将结果与标准药物甲硝唑进行了比较。一般来说,钯配合物表现出比其相应配体更好的活性。与甲硝唑的 IC₅₀ = 1.82 μM 相比,化合物 3a 表现出更好的 IC₅₀ = 0.05 μM。