作为抗疟剂的2,4,6-三取代嘧啶的合成。
Synthesis of 2,4,6-trisubstituted pyrimidines as antimalarial agents.
作者信息
Agarwal Anu, Srivastava Kumkum, Puri S K, Chauhan Prem M S
机构信息
Division of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
出版信息
Bioorg Med Chem. 2005 Aug 1;13(15):4645-50. doi: 10.1016/j.bmc.2005.04.061.
PMID:15896965
Abstract
A series of 2,4,6-trisubstituted-pyrimidines were synthesized and evaluated for their in vitro antimalarial activity against Plasmodium falciparum. Of the 18 compounds synthesized, 14 compounds have shown MIC in the range of 0.25-2 microg/mL. These compounds are in vitro severalfold more active than pyrimethamine.
摘要
合成了一系列2,4,6-三取代嘧啶，并对其针对恶性疟原虫的体外抗疟活性进行了评估。在合成的18种化合物中，有14种化合物的最低抑菌浓度（MIC）在0.25-2微克/毫升范围内。这些化合物在体外的活性比乙胺嘧啶高几倍。
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