一些取代吡唑衍生物作为抗原虫剂的合成

M. Verma, V. Gupta, R. Nema, U. Misra
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引用次数: 0

摘要

含有吡唑片段的化合物由于其模板作为有用的药物分子支架的治疗效用而吸引了大量的研究。我们报道了在环的第5位被苯胺取代的吡唑部分作为抗原生动物的先导部分的合成。对所有化合物进行了抗原虫活性筛选。化合物3a, 3-氨基-5苯基氨基-4 h -吡唑-4-羧酸乙酯和3c -氨基-5-(-4-甲氧基苯基氨基)-4 h -吡唑-4-羧酸乙酯对恶性疟原虫的IC50值分别为0.132imol/l和0.150imol/l,对多诺瓦利什曼原虫的IC50值分别为0.132imol/l和0.168 imol/l,具有较好的抗疟和抗利什曼原虫活性。该结果为利用吡唑模板作为药效团的一部分设计新型抗原虫双抑制剂开辟了新的途径。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of some substituted pyrazole derivatives as antiprotozoal agents
Compounds incorporating a pyrazole moiety have attracted a great deal of research owing to its therapeutic utility of the templates as useful drug molecule scaffolding. We report the synthesis of Pyrazoles moiety substituted with anilines at the fifth position of the ring as anti-protozoal lead moiety. All the compounds were screened for the anti-protozoal activity. The compounds 3a, 3-Amino-5phenylamino-4H-pyrazole-4-carboxylic acid ethyl ester and 3c 3-Amino-5-(-4- methoxy-phenyl amino)-4H-pyrazole-4-carboxylic acid ethyl ester showed better antimalarial as well as anti-leishmanial activity with IC50 value of 0.132imol/l and 0.150imol/l against P.falciparum and IC50 value of 0.132imol/l and 0.168 imol/l against Leishmaniasis donovani. The result opens up new avenues in designing novel anti-protozoal drugs as dual inhibitor with utilization of pyrazole template as part of the pharmacophore.
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