Synthesis and anti-parasitic activity of C-benzylated (N-arylcarbamoyl)alkylphosphonate esters
2017
Adeyemi, Christiana M. | Isaacs, Michelle | Mnkandhla, Dumisani | Klein, Rosalyn | Hoppe, Heinrich C. | Krause, Rui W.M. | Lobb, Kevin A. | Kaye, Perry T.
Unexpected substituent-dependent regioselectivty challenges in the synthesis of C-benzylated (N-arylcarbamoyl)phosphonate esters have been resolved. The C-benzylated N-furfurylcarbamoyl derivative showed low micromolar PfLDH inhibition, while one of the C-benzylated N-arylcarbamoyl analogues was active against Nagana Trypanosoma brucei parasites which are responsible for African trypanosomiasis in cattle.
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