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基曼尼希基衍生物:合成,抗疟疾活动对抗Plasmodium knowlesi,以及分子对接分析

Jufrizal Syahri¹, Rahmiwati Hilma¹, Amatul Hamizah Ali²

¹Department of Chemistry, Universitas Muhammadiyah Riau Jalan Tuanku Tambusai Ujung Pekanbaru Indonesia jsyachri@umri.ac.id.

|December 13, 2023

概括

新的石墨烯衍生物显示出作为抗疟疾药物对抗抗性虫寄生虫的承诺. 这些化合物表现出强烈的活性和高选择性,向二叶酸还原酶-甲基酸合成酶 (PfDHFR-TS).

科学领域:

药用化学医学化学
寄生虫学的寄生虫学
药物发现药物发现药物发现

背景情况:

寄生虫的抗药性需要新的抗疟疾药物.
修改 chalcones 上的氨基组替代物可以增强抗疟疾活性并减少交叉耐药性.

研究的目的:

为了合成具有氨基基群的新型石墨烯衍生物.
评估它们对Plasmodium knowlesi和Plasmodium falciparum的抗疟疾活性.
为了研究它们与Plasmodium falciparum二二酸盐减少酶-二基酸合成酶 (PfDHFR-TS) 的分子相互作用.

主要方法:

通过曼尼赫式反应合成石墨烯衍生物.
在体外对P. knowlesi和P. falciparum进行抗疟疾活性测试.
对抗PfDHFR-TS的分子对接模拟.

主要成果:

卡尔曼尼赫型基衍生物2a,2e和2h在P. knowlesi和P. falciparum的体外显示出强大的抗疟活性.
化合物2a,2e和2h对两种寄生虫菌株都表现出高选择性指数 (SI>10).
分子对接揭示了化合物2a,2e和2h与PfDHFR-TS.的强有力的结合亲缘关系 (CDOCKER能量).

结论:

基曼尼赫型基衍生物2a,2e和2h具有显著的抗疟疾潜力.
PfDHFR-TS被确定为这些新型化合物的可能分子标.
这项研究支持开发这些衍生品作为新的抗疟疾药物候选药物.

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