Antimalarial activity and docking studies of novel bi-functional hybrids derived from 4-aminoquinoline and 1,3,5-triazine against wild and mutant malaria parasites as pf-DHFR inhibitor

作者：Bhat Hans Raj^*; Singh Udaya Pratap; Gahtori Prashant; Ghosh Surajit Kumar; Gogoi Kabita; Prakash Anil; Singh Ramendra K

来源：RSC Advances, 2013, 3(9): 2942-2952.

DOI：10.1039/c2ra21915h

Bi-functional conjugates comprised of 4-aminoquinoline and 1,3,5-triazine were synthesized through facile synthetic routes. These compounds were rigorously screened for determination of their antimalarial activity against wild and mutant cultured Plasmodium falciparum. The results disclosed that the conjugates have considerable antimalarial activity against both wild and mutant parasites with marked variation on changing the pattern of substitutions. The observed activity profiles were additionally substantiated by docking studies on both wild and quadruple mutant P. falciparum dihydrofolate reductase thymidylate synthase (pf-DHFR-TS).

• 出版日期2013