发明名称 |
BROAD SPECTRUM ANTIBIOTIC ARYLOMYCIN ANALOGS |
摘要 |
<p>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 spectum 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.</p> |
申请公布号 |
WO2012036907(A2) |
申请公布日期 |
2012.03.22 |
申请号 |
WO2011US49967 |
申请日期 |
2011.08.31 |
申请人 |
ROMESBERG, FLOYD E.;SMITH, PETER A.;ROBERTS, TUCKER C. |
发明人 |
ROMESBERG, FLOYD E.;SMITH, PETER A.;ROBERTS, TUCKER C. |
分类号 |
C07K5/12 |
主分类号 |
C07K5/12 |
代理机构 |
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地址 |
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