Novel 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidine derivatives and their antitrypanosomal activities against T.brucei,Bioorganic & Medicinal Chemistry Letters

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Novel 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidine derivatives and their antitrypanosomal activities against T.brucei
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2024-05-31 , DOI: 10.1016/j.bmcl.2024.129825
Annie E Taylor ₁ , Moritz Hering ₁ , Mark R J Elsegood ₂ , Simon J Teat ₃ , George W Weaver ₂ , Randolph R J Arroo ₄ , Marcel Kaiser ₅ , Pascal Maeser ₅ , Avninder S Bhambra ₁

Affiliation

Human African trypanosomiasis, or sleeping sickness, is a neglected tropical disease caused by and and is invariably fatal unless treated. Current therapies present limitations in their application, parasite resistance, or require further clinical investigation for wider use. Our work, informed by previous findings, presents novel 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidine derivatives with promising antitrypanosomal activity. In particular, exhibits an EC value of 0.5 µM against , and analogues , and show antitrypanosomal activities in the <1 µM range. We have demonstrated that substituted 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidines present promising antitrypanosomal hit molecules with potential for further preclinical development.

中文翻译：

新型4-[4-(4-甲基哌嗪-1-基)苯基]-6-芳基嘧啶衍生物及其对布氏锥虫的抗锥虫活性

非洲人类锥虫病，或称昏睡病，是一种被忽视的热带疾病，由非洲锥虫病引起，如果不接受治疗，总是致命的。目前的疗法在应用、寄生虫抗性方面存在局限性，或者需要进一步的临床研究才能更广泛地使用。我们的工作根据之前的发现，提出了具有良好抗锥虫活性的新型 4-[4-(4-甲基哌嗪-1-基)苯基]-6-芳基嘧啶衍生物。特别是，对、和类似物的 EC 值为 0.5 µM，并在 <1 µM 范围内表现出抗锥虫活性。我们已经证明，取代的 4-[4-(4-甲基哌嗪-1-基)苯基]-6-芳基嘧啶是有前景的抗锥虫命中分子，具有进一步临床前开发的潜力。

更新日期：2024-05-31

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