4-氨基喹啉-1,3,5-三嗪杂化衍生物的合成、抗疟活性及分子对接
Synthesis, antimalarial activity and molecular docking of hybrid 4-aminoquinoline-1,3,5-triazine derivatives.
作者信息
Bhat Hans Raj, Singh Udaya Pratap, Thakur Anjali, Kumar Ghosh Surajit, Gogoi Kabita, Prakash Anil, Singh Ramendra K
机构信息
Department of Pharmaceutical Sciences, Sam Higginbottom Institute of Agriculture, Technology & Science, Deemed University, Allahabad 211007, India.
Department of Pharmaceutical Sciences, Sam Higginbottom Institute of Agriculture, Technology & Science, Deemed University, Allahabad 211007, India; Nucleic Acids and Antiviral Research Laboratory, Department of Chemistry, University of Allahabad, Allahabad 211002, India.
出版信息
Exp Parasitol. 2015 Oct;157:59-67. doi: 10.1016/j.exppara.2015.06.016. Epub 2015 Jul 9.
A series of novel hybrid 4-aminoquinoline 1,3,5-triazine derivatives was synthesized in a five-steps reaction and evaluated for their in vitro antimalarial activity against chloroquine-sensitive (3D7) and chloroquine-resistant (RKL-2) strains of Plasmodium falciparum. Entire synthetic derivatives showed higher antimalarial activity on the sensitive strain while two compounds, viz., 9a and 9c displayed good activity against both the strains of P. falciparum. The observed activity was further substantiated by docking study on both wild and qradruple mutant type P. falciparum dihydrofolate reductase-thymidylate synthase (pf-DHFR-TS).
通过五步反应合成了一系列新型杂化4-氨基喹啉-1,3,5-三嗪衍生物，并对其针对恶性疟原虫氯喹敏感株（3D7）和氯喹耐药株（RKL-2）的体外抗疟活性进行了评估。所有合成衍生物对敏感株均表现出较高的抗疟活性，而两种化合物，即9a和9c，对恶性疟原虫的两种菌株均显示出良好活性。通过对野生型和四重突变型恶性疟原虫二氢叶酸还原酶-胸苷酸合成酶（pf-DHFR-TS）进行对接研究，进一步证实了观察到的活性。
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