从合成万古霉素类似物的构效关系研究中鉴定强效广谱抗生素。
Identification of potent and broad-spectrum antibiotics from SAR studies of a synthetic vancomycin analogue.
作者信息
Ahrendt Kateri A, Olsen Jacob A, Wakao Masahiro, Trias Joaquim, Ellman Jonathan A
机构信息
Center for New Directions in Organic Synthesis, Department of Chemistry, University of California, Berkeley 94720, USA.
出版信息
Bioorg Med Chem Lett. 2003 May 19;13(10):1683-6. doi: 10.1016/s0960-894x(03)00243-9.
Dimeric vancomycin analogues based on a lead compound identified from a library of synthetic analogues of vancomycin have up to 60-fold greater activity than vancomycin against vancomycin-resistant Enterococcus faecium (VRE, VanA phenotype). Simplified analogues have also been prepared and found to maintain activity against VRE and have broad-spectrum antibiotic activity.
基于从万古霉素合成类似物文库中鉴定出的先导化合物的二聚体万古霉素类似物，对耐万古霉素屎肠球菌（VRE，VanA表型）的活性比万古霉素高60倍。还制备了简化类似物，发现其对VRE保持活性并具有广谱抗生素活性。
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