| 摘要 |
Provided are compounds, the use of the said compounds in treatment, for example treatment of microbial infections, particularly by Gram negative bacteria. The compounds are polymyxin-based and are represented by the formula (I):;and pharmaceutically acceptable salts thereof, where X is —NHC(O)—, —C(O)—, —OC(O)—, —CH2— or —SO2—; R5 represents C0-12 alkyl(C4-6 heterocyclyl), or C2-12 alkyl or C0-12 alkyl(C3-8 cycloalkyl). and the alkyl or cycloalkyl bears one, two or three hydroxyl groups, or a —NR6R7 group, or one —NR6R7 group and one or two hydroxyl groups; and R1 to R4 and R6 to R8 are as defined in the description. |
| 主权项 |
1. A compound of the formula (I): wherein: X represents an —NHC(O)—, —C(O)—, —OC(O)—, —CH2— or —SO2—; and R1 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, represents a phenylalanine, leucine or valine residue; R2 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, represents a leucine, iso-leucine, phenylalanine, threonine, valine or nor-valine residue; R3 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, represents a threonine or leucine residue; R4 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, represents α,γ-diaminobutyric acid or a serine residue; R5 represents
C0-12 alkyl(C4-6 heterocyclyl), orC2-12 alkyl or C0-12 alkyl(C3-8 cycloalkyl) wherein the alkyl or cycloalkyl bears:
i) one, two or three hydroxyl groups, orii) a —NR6R7 group, oriii) one —NR6R7 group and one or two hydroxyl groups, R6 represents hydrogen or C1-4 alkyl; and R7 represents hydrogen or C1-4 alkyl, R8 represents hydrogen or methyl, or a pharmaceutically acceptable salt thereof. |
