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- Title
Synthesis, Docking, In Vitro and In Vivo Antimalarial Activity of Hybrid 4-aminoquinoline-1,3,5-triazine Derivatives Against Wild and Mutant Malaria Parasites.
- Authors
Bhat, Hans Raj; Singh, Udaya Pratap; Gahtori, Prashant; Ghosh, Surajit Kumar; Gogoi, Kabita; Prakash, Anil; Singh, Ramendra K.
- 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, 3 QG2.pdb) type pf- DHFR- TS to highlight the structural features of hybrid molecules.
- Subjects
DRUG synthesis; ANTIMALARIALS; TRIAZINE derivatives; AROMATIC compound synthesis; MOLECULAR docking; DRUG resistance in bacteria; THERAPEUTICS
- Publication
Chemical Biology & Drug Design, 2015, Vol 86, Issue 3, p265
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12490