Abstract:Fluorene-chloroquine hybrids have been identified as a new promising class of antiplasmodial agents. The most active compound 9 d exhibited good in vitro antiplasmodial activity against a chloroquine-sensitive NF54 strain of the human malaria parasite Plasmodium falciparum with an IC 50 value of 139 nM. UV-visible absorption, FTIR spectral and 1 H NMR titration data corroborated the binding of 9 d to monomeric and μ-oxodimeric heme as well as inhibition of β-hematin formation, which collectively supported the … Show more
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