Antiplasmodial activity of piperazine sulfonamides

A high-throughput screening program identified two piperazine sulfonamides with activity against Plasmodium falciparum. Both screening positives had three structural features with potential liabilities: furanyl, thiourea and nitrophenyl groups. The furan could be replaced with no loss of activity, replacement of the nitrophenyl led to some loss of activity, and any attempt to replace the thiourea led to a significant decrease in activity, which implicates this reactive functional group’s role in the antiplasmodial activity of this compound class.

Graphical abstractThe synthesis and antiplasmodial activity of analogs based on piperazine sulfonamides screening positives 1a–b is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide