Article
Synthesis, docking and in vitro antimalarial evaluation of bifunctional hybrids derived from β-lactams and 7-chloroquinoline using click chemistry.
Bioorganic & medicinal chemistry letters - 1 Jan 2012
Singh Pardeep, Singh Parvesh, Kumar Malkeet, Gut Jiri, Rosenthal Philip J, Kumar Kewal, Kumar Vipan, Mahajan Mohinder P, Bisetty Krishna
Abstract excerpt
1,2,3-Triazole tethered β-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 β-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...
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