Antiplasmodial activity of piperazine sulfonamides

Bioorganic & Medicinal Chemistry Letters
Derek C MartynJon Clardy

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.

References

Apr 12, 2000·Biochemistry·L K LightningW F Trager
Jun 25, 2005·Current Drug Metabolism·Amit S KalgutkarShawn P Harriman
Nov 23, 2006·Antimicrobial Agents and Chemotherapy·Mary Lynn BanieckiJon Clardy

Citations

Jun 7, 2012·Parasitology International·Pablo Bilbao-RamosM Eugenia González-Rosende
Aug 9, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·D I UgwujaD I Ugwu
Oct 4, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Veronika R KarpinaLouis Maes
Feb 21, 2021·European Journal of Medicinal Chemistry·William NguyenBrad E Sleebs
Apr 17, 2013·Bioorganic & Medicinal Chemistry Letters·Marco A BiamonteKarine G Le Roch

Related Concepts

Piperazine tartrate (1: 1), (R-(R*, R*))-isomer
Furan
Antimalarials
Tetrahydrofurans
Piperazines
Plasmodium falciparum
Sulfonamides
Thiourea
High-Throughput Chemical Assays
Immunoglobulin Isotypes

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