【文章名】Synthesis, docking and in vitro antimalarial evaluation of bifunctional hybrids derived from beta-lactams and 7-chloroquinoline using click chemistry
[摘要]：1,2,3-Triazole tethered beta-lactam and 7-chloroquinoline bifunctional hybrids were synthesized and evaluated as potential antimalarial agents. Activity against cultured Plasmodium falciparum was dependent on the N-substituent of the beta-lactam ring as well as the presence of bis-triazole at the C-3 position. The observed activity profiles were further substantiated by docking studies via inhibition of P. falciparum dihydrofolate reductase (PfDHFR), a potential target for the development of new anti-malarials. (C) 2011 Elsevier Ltd. All rights reserved.
