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具有抗质活性的Piperazine绑定的thiazole化合物的并行合成

Ramanjaneyulu Rayala¹, Prakash Chaudhari¹, Ashley Bunnell¹

¹Herbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Miami, FL 33199, USA.

International journal of molecular sciences

|December 23, 2023

概括

研究人员为抗疟疾药物发现合成了新型皮佩拉结合的醇化合物. 一个关键的化合物显示出对抗抗克洛洛昆耐药的Plasmodium falciparum菌株的强有力的活性.

科学领域:

药用化学医学化学
有机合成有机合成
寄生虫学的寄生虫学

背景情况:

thiazole 和 piperazine 是药物和农业化学中至关重要的异环基架.
这些结构在许多天然产品和合成药物中普遍存在.
开发新的衍生品是发现新治疗剂的关键.

研究的目的:

为了合成一系列与皮佩拉结合的醇化合物.
为了评估合成的化合物对抗等离子体活性.
为了确定新的抗疟疾药物候选者.

主要方法:

平行合成与皮佩拉结合的醇衍生物.
皮佩拉与4-甲基-2-氨基醇的反应.
对化合物的查,以检测Plasmodium falciparum Dd2菌株的化合物.

主要成果:

合成化合物的高纯度和良好的产量.
鉴定具有显著抗等离子体活性的化合物.
被击中化合物2291-61的EC50为102nM,对抗抗克洛洛昆的Dd2菌株.
对于被击中化合物来说,选择性指数超过140.

结论:

合成的与皮佩拉结合的提亚醇是抗疟疾药物开发的有前途的化合物类别.
化合物2291-61是一种强效的,具有高选择性对抗Plasmodium falciparum.
对这种化学系列的进一步调查可能会产生有效的疟疾治疗方法.

关键词:

它具有抗等离子体活性.组合化学是一种组合化学.异环化合物异环化合物异环化合物疟疾疟疾是一种疾病.固相合成的固相合成方法蒂亚醇连接的皮佩拉津.

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