title: Antiplasmodial activity of piperazine sulfonamides.
abstract: 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.
authors.affiliation: Broad Institute Infectious Diseases Initiative, 7 Cambridge Center, Cambridge, MA 02142, USA.
authors.forename: Derek C
authors.initials: DC
authors.lastname: Martyn
authors.forename: Joseph F
authors.initials: JF
authors.lastname: Cortese
authors.forename: Erin
authors.initials: E
authors.lastname: Tyndall
authors.forename: Justin
authors.initials: J
authors.lastname: Dick
authors.forename: Ralph
authors.initials: R
authors.lastname: Mazitschek
authors.forename: Benito
authors.initials: B
authors.lastname: Munoz
authors.forename: Jon
authors.initials: J
authors.lastname: Clardy
mesh_terms: 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
chemical_list: D000962:Antimalarials; D005663:Furans; D010879:Piperazines; D013449:Sulfonamides; D000077489:Piperazine; D013890:Thiourea; C039281:furan