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嘧啶结构骨架类抗疟药研究进展

         

摘要

Pyrimidine structural skeleton is one of the most important pharmacophore in the history of anti-malaria,which is widely concerned because it has a variety of pharmacological activities and is easier to synthesize and reform.In the recent years,some traditional antimalarial drugs have emerged in resistance. The effect of treatmenthas been significantly decreasing, so the modification of traditional antimalarial drugs has become imperative. In this paper, the recent novel pyrimidine skeleton compounds on antimalaria,such as benzopyrimidine, aminopyrimidine, quinoline pyrimidine and thiophene pyrimidine, are reviewed and this will provide some reference for the design of new antimalarial drugs.%嘧啶结构骨架是抗疟史上最为重要的药效团之一,因其具有多种药理活性且较易于合成与改造而受到广泛的关注.近年来,部分传统的抗疟药物已出现了耐药性,治疗效果明显降低,因此对传统抗疟药物进行结构修饰已势在必行.对近10年来发现的新型嘧啶结构骨架化合物(苯并嘧啶、胺基嘧啶、喹啉并嘧啶和噻吩并嘧啶)在结构特征、抗疟活性和构效关系等方面进行了综述,以期为新型抗疟药的设计提供一些参考.

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