el-Sabbagh Osama I, Rady Hanaa M
Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.
Eur J Med Chem. 2009 Sep;44(9):3680-6. doi: 10.1016/j.ejmech.2009.04.001. Epub 2009 Apr 8.
Cyclic beta-diketone namely, dimedone was utilized to prepare different chemical entities whether cyclic such as acridines, thiadiazole and triazole or acyclic systems as hydrazide, hydrazones, thiosemicarbazide and semicarbazide. The structures of the novel compounds were determined using elemental analyses and various spectroscopic methods. Most acyclic derivatives especially semicarbazide 19, hydrazide 9 and thiosemicarbazide 16 showed a higher in vitro cytotoxic activity against hepatoma cell line (HepG2) than the cyclized acridine derivatives. The antiviral activity of the new compounds against Hepatitis A Virus (HAV) using the plague infectivity reduction assay revealed that the acridine 4 and the hydrazone 12 were more active than the reference drug amantadine.
环状β-二酮即达米东，被用于制备不同的化学实体，无论是环状的如吖啶、噻二唑和三唑，还是非环状体系如酰肼、腙、硫代氨基脲和氨基脲。通过元素分析和各种光谱方法确定了新型化合物的结构。大多数非环状衍生物，尤其是氨基脲19、酰肼9和硫代氨基脲16，对肝癌细胞系（HepG2）的体外细胞毒性活性高于环化的吖啶衍生物。使用蚀斑感染性降低试验对新化合物抗甲型肝炎病毒（HAV）的抗病毒活性进行检测，结果显示吖啶4和腙12比参比药物金刚烷更具活性。
