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  • Title: Synthesis, docking and in vitro antimalarial evaluation of bifunctional hybrids derived from β-lactams and 7-chloroquinoline using click chemistry.
    Author: Singh P, Singh P, Kumar M, Gut J, Rosenthal PJ, Kumar K, Kumar V, Mahajan MP, Bisetty K.
    Journal: Bioorg Med Chem Lett; 2012 Jan 01; 22(1):57-61. PubMed ID: 22172698.
    Abstract:
    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 dihydrofolate reductase (PfDHFR), a potential target for the development of new anti-malarials.
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