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Bioorganic & medicinal chemistry letters DOI:10.1016/j.bmcl.2009.10.130

Antiplasmodial activity of piperazine sulfonamides.

Publication TypeJournal Article
Year of Publication2010
AuthorsMartyn, DC, Cortese, JF, Tyndall, E, Dick, J, Mazitschek, R, Munoz, B, Clardy, J
JournalBioorganic & medicinal chemistry letters
Volume20
Issue1
Pages218-21
Date Published2010/01/01
ISSN0960-894X
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.

URLhttp://linkinghub.elsevier.com/retrieve/pii/S0960-894X(09)01551-0
DOI10.1016/j.bmcl.2009.10.130
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/19914069?dopt=Abstract