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2-[3,5-取代吡唑-1-基]-4,6-三取代三嗪衍生物作为抗疟剂的合成

Synthesis of 2-[3,5-substituted pyrazol-1-yl]-4,6-trisubstituted triazine derivatives as antimalarial agents.

作者信息

Katiyar Sanjay Babu, Srivastava Kumkum, Puri S K, Chauhan Prem M S

机构信息

Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.

出版信息

Bioorg Med Chem Lett. 2005 Nov 15;15(22):4957-60. doi: 10.1016/j.bmcl.2005.08.023.

Abstract

A series of 22 compounds were synthesized and screened against Plasmodium falciparum NF-54 strain. Of the screened compounds, 6 compounds showed MIC in the range between 1 and 2 microg/mL. These compounds are 32 times more potent than the cycloguanil which was used as the standard drug.

摘要

合成了一系列22种化合物,并针对恶性疟原虫NF-54株进行了筛选。在筛选出的化合物中,有6种化合物的最低抑菌浓度在1至2微克/毫升之间。这些化合物的效力是用作标准药物的环氯胍的32倍。

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