Patent ID: 6495663
Filing Date: 2002-12-17
Classification: A61K,A61P,C07B,C07D,C40B

Abstract:
A conjugate for administration, to a mammalian subject, of an antimicrobial agent whose efficacy in non-conjugated form is limited by its solubility in aqueous liquid or its inability to cross biological membranes to manifest biological activity, said conjugate comprises a transport peptide covalently attached by a linker to the antimicrobial agent, said linker being cleaved in vivo to release the antimicrobial agent from the linker and the transport peptide, wherein the attached transport peptide:(a) consists of from 6 to 25 amino acid residues, at least 50% of which contain a guanidino sidechain having the structure or an amidino sidechain having the structure wherein n is 2, 3, 4 or 5;(b) contains at least 6 contiguous amino acid residues containing said guanidino or amidino sidechain; and (c) increases the delivery of the antimicrobial agent across a biological membrane relative to the delivery of the antimicrobial agent in non-conjugated form.