首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Probing the antiamoebic and cytotoxicity potency of novel tetrazole and triazine derivatives.
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Probing the antiamoebic and cytotoxicity potency of novel tetrazole and triazine derivatives.

机译:探索新型四唑和三嗪衍生物的抗厌氧和细胞毒性能力。

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摘要

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.
机译:合成了一系列带有四唑和三嗪环基序与SO(2)NH功能共轭的化合物,并研究了它们的抗厌氧效力。检查化合物对人肝癌细胞系HepG2的细胞毒性。引入三嗪环代替四唑导致该化合物的抗厌氧活性急剧增加。发现所研究化合物的抗厌氧活性是位置和取代基依赖性的。体外细胞毒性结果显示,所有浓度高达25?μM的化合物均具有非细胞毒性。获得的化合物5c和5d具有最低的细胞毒性(IC(50)→> 100?μM)和出色的解组织变形虫抑制剂,其IC(50)值分别为1.05?μM和1.02?μM。

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