Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia (Central, University), New Delhi 110025, India.
Eur J Med Chem. 2012 Feb;48:313-20. doi: 10.1016/j.ejmech.2011.12.033. Epub 2011 Dec 30.
A series of compounds bearing a Tetrazole and Triazine ring motif conjugated with a SO(2)NH function were synthesized and investigated for their antiamoebic potency. Cytotoxicity of the compounds was checked on human hepatocellular carcinoma cell line HepG2. Incorporation of Triazine ring in place of tetrazole resulted in a precipitous increase in the antiamoebic activity of the compounds. Antiamoebic activity of the investigated compounds was found to be position and substituent dependent. In vitro cytotoxicity results revealed noncytotoxic nature of all the tested compounds up to a concentration of 25 μM. Compound 5c and 5d were obtained as least cytotoxic (IC(50) > 100 μM) and excellent Entamoeba histolytica inhibitors with IC(50) values of 1.05 μM and 1.02 μM respectively.
一系列含有四唑和三嗪环结构并与 SO(2)NH 功能共轭的化合物被合成并研究了它们的抗变形虫活性。在人肝癌细胞系 HepG2 上检查了化合物的细胞毒性。用三嗪环代替四唑会导致化合物的抗变形虫活性急剧增加。研究化合物的抗变形虫活性发现与位置和取代基有关。体外细胞毒性结果表明，所有测试化合物在高达 25 μM 的浓度下均无细胞毒性。化合物 5c 和 5d 的细胞毒性最低（IC(50) > 100 μM），是优秀的溶组织内阿米巴抑制剂，IC(50) 值分别为 1.05 μM 和 1.02 μM。
