| 摘要 |
Novel peptide compounds and pharmaceutical compositions thereof are disclosed that have a formula represented by the following formula (I) wherein L1, L2, L3, Z, R1, R2, R4 and R5 are as described herein. The compounds demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention and treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present peptides are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provided by standard antibiotics.; |
| 主权项 |
1. A pharmaceutical composition for treating or managing a disease or condition caused by bacteria; wherein the pharmaceutical composition comprises a peptide according to formula I: wherein L1 is independently unsubstituted C2-5 alkylene; L2 is unsubstituted C3-5 alkylene; each R1 is independently —NH—WR—Z, —NH—RW—Z, —NH—RF—Z, —NH—FR—Z, —NH—RY—Z, —NH—YR—Z, —NH—KW—Z, —NH—WK—Z, —NH—KY—Z, —NH—YK—Z, —NH—KF—Z, —NH—FK—Z, —NH—RWW—Z, —NH—RFF—Z, —NH—RYY—Z, —NH—KWW—Z, —NH—KYY—Z, —NH—KFF—Z, —NH—WWR—Z, —NH—FFR—Z, —NH—YYR—Z, —NH—WWK—Z, —NH—YYK—Z, or —NH—FFK—Z, or m is 1, 2, 3, or 4; each Z is independently H, Ac, or any other conventional N-protecting group;R3 is unsubstituted alkyl, aralkyl, heteroarylalkyl, aminoalkyl, or guanidinoalkyl; R2 is R1; or R2 is —N(L1-R1)2;
andTta is 2,5,7-trialkyltryptophan residue; or a pharmaceutically acceptable salt thereof. |
