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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and antiamoebic activity of metronidazole thiosemicarbazone analogues.
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Synthesis and antiamoebic activity of metronidazole thiosemicarbazone analogues.

机译：甲硝唑硫代半碳胺类似物的合成及其抗厌氧活性。

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Repeated treatment of Entamoeba histolytica infection with commonly used antiamoebic drugs results in not only increasing the toxicity potential but also leads to the development of clinical resistance. Thus new effective agents with less toxicity against amoebiasis are urgently required. With this view, metronidazole thiosemicarbazone analogues 1-11 were synthesized wherein thioamide moiety was substituted by different cyclic and aromatic amines. These compounds were screened against HM1:IMSS strain of E. histolytica parasite cultured in vitro and the sensitivity of the parasite to the metronidazole thiosemicarbazones was evaluated using the microdilution method. Eight compounds (1-4, 7-9 and 11) were found better inhibitors of E. histolytica growth since IC50 values elicited by these compounds were much lower than metronidazole with compound 4 showing the most promising antiamoebic activity (IC50=0.56 microM). The study suggests the beneficial potential of these leads that need to be further exploredin order to discover and develop better and yet safer therapeutic agents for amoebiasis.
机译：用常用的抗阿米巴药物反复治疗溶血性变形杆菌，不仅会增加毒性潜能，而且还会导致临床耐药性的发展。因此，迫切需要对阿米巴病毒性较小的新型有效药物。从该观点出发，合成了甲硝唑硫半脲酮类似物1-11，其中硫酰胺部分被不同的环状和芳族胺取代。针对体外培养的溶组织性大肠杆菌的HM1：IMSS菌株筛选了这些化合物，并使用微量稀释方法评估了该寄生虫对甲硝唑硫代半氨基甲酮的敏感性。发现八种化合物（1-4、7-9和11）是更好的溶血性大肠杆菌生长抑制剂，因为这些化合物引起的IC50值远低于甲硝唑，其中化合物4表现出最有希望的抗厌氧活性（IC50 = 0.56 microM）。该研究表明，这些线索的有益潜力需要进一步探索，以发现和开发更好，更安全的阿米巴病治疗药物。

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