Synthesis and anti-protozoal activity of C2-substituted polyazamacrocycles

A focused library of C2-substituted-1,4,7,10-tetraazacyclododecanes was synthesised and the compounds were tested for their ability to kill trypanosome and malaria parasites. Several compounds showed significant in vitro activity and were selectively active against the parasites over human embryonic kidney cells used as a counter screen.

Graphical abstractA focused library of C2-substituted-1,4,7,10-tetraazacyclododecanes have been synthesized and shown to have significant in vivo anti-protozoal activity against both trypanosome and malaria parasites.Figure optionsDownload full-size imageDownload as PowerPoint slide