Design and synthesis of novel triazine derivatives as antimalarial agents

IF 2.2 4区 医学 Q3 CHEMISTRY, MEDICINAL Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-04-01 Epub Date: 2024-12-28 DOI:10.1016/j.bmcl.2024.130091
Yuko Asamitsu , Aki Ishiyama , Yui Iwamae , Rina Nagao , Rei Hokari , Masato Iwatsuki , Kazuhiko Otoguro , Masaaki Sawa
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Abstract

In a previous study, we reported that nilotinib, a BCR-ABL tyrosine kinase inhibitor, possesses moderate antimalarial activity against PfK1 and PfFCR3. As a part of our efforts to develop novel antimalarial agents, a series of novel triazine analogs was identified as potent antimalarial agents via structure modification of nilotinib. Compound 15a showed strong antimalarial activities against PfK1 and PfFCR3 with IC50 values of 0.28 and 0.29 µM, respectively.

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新型抗疟药三嗪衍生物的设计与合成。
在之前的研究中,我们报道了尼罗替尼,一种BCR-ABL酪氨酸激酶抑制剂,对PfK1和PfFCR3具有中等的抗疟疾活性。作为我们开发新型抗疟药物的一部分,通过对尼洛替尼的结构修饰,发现了一系列新的三嗪类似物作为有效的抗疟药物。化合物15a对PfK1和PfFCR3具有较强的抗疟活性,IC50值分别为0.28和0.29 µM。
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来源期刊
CiteScore
5.70
自引率
3.70%
发文量
463
审稿时长
27 days
期刊介绍: Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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