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ID: ALA1135031

Journal: Bioorg Med Chem Lett

Title: Sequestration of bacterial lipopolysaccharide by bis(Args) gemini compounds.

Authors: David S, Pérez L, Infante MR.

Abstract: Gemini compounds of the type N(alpha),N(omega)-bis(N(alpha)-lauroyl arginine)alpha,omega-alkylenediamides or bis(Args) bind bacterial lipopolysaccharide and neutralize endotoxic activity in in vitro tumor necrosis factor-alpha 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.

CiteXplore: 11814796

DOI: 10.1016/s0960-894x(01)00749-1