Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, Maulana Ali Jauhar Marg, New Delhi-110025, India.
Eur J Med Chem. 2012 Aug;54:845-54. doi: 10.1016/j.ejmech.2012.03.049. Epub 2012 Apr 3.
A series of pyrazoline derivatives (1a-15a) was synthesized by cyclization of chalcones (1-15) with 2-[5-(4-methoxyphenyl)-1H-tetrazol-1-yl]acetohydrazide under basic conditions and were screened in vitro, to find out effect on the growth of HM1: IMSS strain of Entamoeba histolytica. The compounds 3a, 4a, 11a, 13a and 14a showed encouraging results with IC(50) value in the range of 0.86-1.28 μM. However compound 13a showed most promising results with IC(50) = 0.86 μM which is half of the metronidazole, the standard drug used for protozoal infection. Cell viability test in human hepatocellular carcinoma cell line (HepG2) revealed non-toxic nature of new synthesized compounds. Safety index calculations prevailed compound 13a as highly antiamoebic and least cytotoxic (S.I. = >116.28), almost twice than metronidazole.
通过 chalcones（1-15）与 2-[5-(4-甲氧基苯基)-1H-四唑-1-基]乙酰肼在碱性条件下环化，合成了一系列吡唑啉衍生物（1a-15a），并在体外筛选，以发现对 HM1：IMSS 株溶组织内阿米巴生长的影响。化合物 3a、4a、11a、13a 和 14a 表现出令人鼓舞的结果，IC50 值在 0.86-1.28 μM 范围内。然而，化合物 13a 表现出最有前途的结果，IC50 = 0.86 μM，是用于原生动物感染的标准药物甲硝唑的一半。在人肝癌细胞系（HepG2）中的细胞活力测试表明，新合成的化合物具有非毒性。安全指数计算表明，化合物 13a 具有高度抗阿米巴作用和最小的细胞毒性（S.I.>116.28），几乎是甲硝唑的两倍。
