| 摘要 |
<p>The present invention provides sensitizers and antimicrobial compositions comprising an antibiotic and a sensitizer that enhances the effectiveness or activity of the antibiotic, wherein the sensitizer is preferably a disulfide cyclized analogue of a polymyxin nonapeptide. The disulfide cyclized analogue is characterized by: in which X represents a natural or unnatural hydrophobic D-amino acid; Y represents a natural or unnatural hydrophobic L-amino acid, threonine or serine, or, alternatively, where X and Y together represent a dipeptide isostere or turn mimetic; R1 represents a hydrogen atom, an alkyl group, an amino acid or a dipeptide; and R2 represents H, NH2, NHR3, (NR3)2,R3, OH or OR3, in which R3 is an alkyl group, an amino acid or a dipeptide. Compositions containing the sensitizer of the invention are particularly useful for the treatment of infections by drug resistant bacteria.</p> |
