发明名称 |
BROAD SPECTRUM ANTIBIOTIC ARYLOMYCIN ANALOGS |
摘要 |
Arylomycin analogs are provided, wherein the analogs can have broad spectrum bioactivity. Resistance to the antibiotic bioactivity of natural product arylomycin in a range of pathogenic bacterial species has been found to depend upon single amino acid mutations at defined positions of bacterial Signal Peptidases (SPases), wherein the presence of a proline residue confers arylomycin resistance. Arylomycin analogs are provided herein that can overcome that resistance and provide for a broader spectrum of antibiotic bioactivity than can natural product arylomycins such as arylomycin A2. Methods for determining if a bacterial strain is susceptible to narrow spectrum arylomycin antibiotics, or if a broad spectrum analog is required for treatment, is provided. Pharmaceutical compositions and methods of treatment of bacterial infections, and methods of synthesis of arylomycin analogs, are provided. |
申请公布号 |
EP2825176(A1) |
申请公布日期 |
2015.01.21 |
申请号 |
EP20130761835 |
申请日期 |
2013.03.08 |
申请人 |
THE SCRIPPS RESEARCH INSTITUTE |
发明人 |
ROMESBERG, FLOYD, E.;SMITH, PETER, A.;ROBERTS, TUCKER, C. |
分类号 |
A61K31/7028 |
主分类号 |
A61K31/7028 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|