Synthesis,Docking, In Vitro and In Vivo Antimalarial Activity of Hybrid 4‐aminoquinoline–1,3,5‐triazine Derivatives Against Wild and Mutant Malaria Parasites |
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| Authors: | Hans Raj Bhat Udaya Pratap Singh Prashant Gahtori Surajit Kumar Ghosh Kabita Gogoi Anil Prakash Ramendra K Singh |
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| Institution: | 1. Drug Design and Discovery Laboratory, Department of Pharmaceutical Sciences, Sam Higginbottom Institute of Agriculture Technology and Science, Deemed University, Allahabad, India;2. Nucleic Acids and Antiviral Research Laboratory, Department of Chemistry, University of Allahabad, Allahabad, India;3. Faculty of Pharmacy, Uttarakhand Technical University, Dehradun, India;4. Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, India;5. Regional Medical Research Centre, ICMR, Dibrugarh, India |
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| Abstract: | A new series of hybrid 4‐aminoquinoline–1,3,5‐triazine derivatives was synthesized by a four‐step reaction. Target compounds were screened for in vitro antimalarial activity against chloroquine‐sensitive (3D‐7) and chloroquine‐resistant (RKL‐2) strains of Plasmodium falciparum. Compounds exhibited, by and large, good antimalarial activity against the resistant strain, while two of them, that is 8g and 8a, displayed higher activity against both the strains of P. falciparum. Additionally, docking study was performed on both wild (1J3I.pdb) and quadruple mutant (N51I, C59R, S108 N, I164L, 3QG2.pdb) type pf‐DHFR‐TS to highlight the structural features of hybrid molecules. |
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| Keywords: | 1 3 5‐triazine aminoquinoline antimalarial docking |
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