Piperazines as antimalarial agents

摘要

The disclosure relates to piperazine derivatives of Formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria. Compounds of the invention include: (S)-N-[4-(4-Acetyl-piperazin-1-yl)-benzyl]-N-{ 1-benzyl-2-[4-(4-cyano-benzyl)-piperazin-1-yl]-2-oxo-ethyl} -3-(4-isopropyl-phenyl)-acrylamide, (S)-N-[4-(4-Acetyl-piperazin-1-yl)-benzyl]-N-{ 1-benzyl-2-[4-(4-cyano-benzyl)-piperazin-1-yl]-2-oxo-ethyl} -3-(4-trifluoromethoxy-phenyl)-acrylamide, (S)-N-[4-(4-Acetyl-piperazin-1-yl)-benzyl]-N-[1-benzyl-2-(4-benzyl-piperazin-1-yl)-2-oxoethyl]-3-(4-ethyl-phenyl)-acrylamide, (S)-N-[4-(4-Acetyl-piperazin-1-yl)benzyl]-N-{ 1-[4-(4-(dimethylamino )benzyl)piperazin-1-yl]-1-oxo-3-phenylpropan-2-yl} -3-(p-tolyl)acrylamide and (S)-N-[4-(4-Acetyl-piperazin-1-yl)-benzyl]-N-{ 1-benzyl-2-[4-(4-dimethylaminobenzyl)piperazin-1-yl]-2-oxo-ethyl} -3-(4-ethoxy-phenyl)-acrylamide,