Synthesis and anti-schistosoma activity of benzodiazepine derivatives

Compound B30 belongs to anxiolytic benzodiazepine derivative.At 50 μM,it exhibits 100% percent anti-schistosomal efficiency in vitro.Employing bioisosteric replacement principle,four B30 analogues 6,10,13,16 was designed and synthesized,and their anti-schistosomal activity in vitro was evaluated.All four compounds displayed certain efficacy.Especially,compound 16 demonstrated substantial worm-killing activity,resulting in 40% worm viable at 50 μM.This research provided alternative structural motif for the new type of anti-schistosomal compounds.