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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and leishmanicidal activities of 1-(4-X-phenyl)-N'-((4-Y-phenyl)methylene)-1H-pyrazole-4-carbohydrazides.
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Synthesis and leishmanicidal activities of 1-(4-X-phenyl)-N'-((4-Y-phenyl)methylene)-1H-pyrazole-4-carbohydrazides.

机译：1-（4-X-苯基）-N′-（（4-Y-苯基）亚甲基）-1H-吡唑-4-碳酰肼的合成和杀人活性。

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摘要

1H-pyrazole-4-carbohydrazides were synthesized and their leishmanicidal in vitro activities and cytotoxic effects were investigated. The drugs prototypes of these new compounds (ketoconazole, benznidazole, allopurinol and pentamidine) were also tested. It was found that among all the 1H-pyrazole-4-carbohydrazides derivatives examined, the most active compounds were those with X = Br, Y = NO2 (27) and X = NO2, Y = Cl (15) derivatives which showed to be most effective on promastigotes forms of L. amazonensis than on L. chagasi and L. braziliensis species. When tested against murine peritoneal macrophages as mammalian host cell controls of toxicity, 1-(4-Br-phenyl)-N'-[(4-NO(2)-phenyl)methylene]-1H-pyrazole-4-carbohydrazid es (27) (EC50 = 50 microM l(-1)) and 1-(4-NO2-phenyl)-N'-[(4-Cl-phenyl)methylene]-1H-pyrazole-4-carbohydrazides (15) EC50 = 80 microM l(-1))] was reasonably toxic. However, both compounds were less toxic than pentamidine and ketoconazole. These results provide new perspectives on the development of drugs with activities against Leishmania parasite.
机译：合成了1H-吡唑-4-碳酰肼，并研究了它们的体外杀菌活性和细胞毒性作用。还测试了这些新化合物的药物原型（酮康唑，苯并咪唑，别嘌呤醇和喷他idine）。发现在所有检查的1H-吡唑-4-碳酰肼衍生物中，活性最高的化合物是X = Br，Y = NO2（27）和X = NO2，Y = Cl（15）的衍生物，表明它们是对亚马逊L. agassonensis的前鞭毛体形式比对L. chagasi和L. braziliensis物种最有效。当针对鼠腹膜巨噬细胞作为哺乳动物的毒性宿主细胞对照进行测试时，1-（4-Br-苯基）-N'-[（4-NO（2）-苯基）亚甲基] -1H-吡唑-4-碳酰肼（ 27）（EC50 = 50 microM l（-1））和1-（4-NO2-苯基）-N'-[（4-Cl-苯基）亚甲基] -1H-吡唑-4-碳酰肼（15）EC50 = 80 microM l（-1））]具有一定毒性。但是，这两种化合物的毒性均不如喷他idine和酮康唑。这些结果为开发具有抗利什曼原虫寄生虫活性的药物提供了新的视角。

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