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.
Martyn
Derek C
DC
Broad Institute Infectious Diseases Initiative, 7 Cambridge Center, Cambridge, MA 02142, USA.
Cortese
Joseph F
JF
Tyndall
Erin
E
Dick
Justin
J
Mazitschek
Ralph
R
Munoz
Benito
B
Clardy
Jon
J
D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005663:Furans / Q000737:chemistry; D057166:High-Throughput Screening Assays; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry*; D010963:Plasmodium falciparum / Q000187:drug effects; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013890:Thiourea / Q000737:chemistry
D000962:Antimalarials; D005663:Furans; D010879:Piperazines; D013449:Sulfonamides; D000077489:Piperazine; D013890:Thiourea; C039281:furan