Abstract
The use of three-component four-center Ugi reactions to afford the synthesis of novel β-lactams is described. Three series of compounds have been made using this reaction in combination with the Mannich reaction. All compounds formed are racemic mixtures and were tested against the chloroquine sensitive D10 strain of Plasmodium falciparum in an in vitro assay. All compounds showed low to moderate microMolar range activity with the most active compounds 2.6 and 3.1 showing IC50 values 16 μM and 15 μM respectively
Highlights
Malaria continues to be a major blight with almost half the world’s population at risk.[1]
The synthesis and antiplasmodial activity of these β-lactams
Series 1 was synthesized from β-alanine, cyclohexyl isocyanide and the chosen aldehyde, Scheme 1
Summary
Malaria continues to be a major blight with almost half the world’s population at risk.[1].
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