| 摘要 |
FIELD: medicine, pharmaceutics. ^ SUBSTANCE: present invention refers to a polymixin derivative, wherein R1, R2 and R3 are optional, but unessential, and R1, R2, R3, R5, R8 and R9 represent cationic or neutral amino acid residues specified so that total positive charge at physiological pH value makes at least two, but no more than three. The invention also refers to a method of treating, relieving or suppressing an infection in an individual caused by a gram-negative bacterium, by introducing a therapeutically effective amount of the derivative according to the present invention to the specified individual; to a method of sensitising the gram-negative bacteria to an antibacterial agent by introducing simultaneously or sequentially in any order the therapeutically effective amount of the specified antibacterial agent and the derivative according to the present invention to the specified individual. ^ EFFECT: developing new antibiotics; reducing nephrotoxicity, improving pharmacokinetic properties of natural polymixins and octapeptines; and sensitising the clinically significant bacteria to the protective mechanism of a host complement found in serum, and also developing a method of producing such polymixin derivatives. ^ 36 cl, 10 tbl, 13 ex |
