Abstract
Gemini compounds of the type Nα,Nω-bis(Nα-lauroyl arginine)α,ω-alkylenediamides or bis(Args) bind bacterial lipopolysaccharide and neutralize endotoxic activity in in vitro tumor necrosis factor-α and nitric oxide release assays. Sequestration of lipopolysaccharide results in protection in a murine model of endotoxemia. However, the bis(Args) compounds are cytotoxic by virtue of being highly membrane-active. The development of less surface-active analogues may yield potentially therapeutically useful compounds for the treatment of Gram-negative sepsis.
Original language | English (US) |
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Pages (from-to) | 357-360 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 12 |
Issue number | 3 |
DOIs | |
State | Published - Feb 11 2002 |
Bibliographical note
Funding Information:This was supported by the MEC, project PPQ2000-1687-CO2-01.