|Publication Type||Journal Article|
|Year of Publication||2010|
|Authors||Martyn, DC, Cortese, JF, Tyndall, E, Dick, J, Mazitschek, R, Munoz, B, Clardy, J|
|Journal||Bioorg Med Chem Lett|
|Date Published||2010 Jan 01|
|Keywords||Antimalarials, Furans, High-Throughput Screening Assays, Piperazines, Plasmodium falciparum, Sulfonamides, Thiourea|
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.
|Alternate Journal||Bioorg. Med. Chem. Lett.|