通过金属配合物的多价抗生素：针对耐万古霉素肠球菌的强效二价万古霉素

Multivalent antibiotics via metal complexes: potent divalent vancomycins against vancomycin-resistant enterococci.

作者信息

Xing Bengang, Yu Chun-Wing, Ho Pak-Leung, Chow Kin-Hung, Cheung Terence, Gu Hongwei, Cai Zongwei, Xu Bing

机构信息

Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Hong Kong, China.

出版信息

J Med Chem. 2003 Nov 6;46(23):4904-9. doi: 10.1021/jm030417q.

DOI:10.1021/jm030417q

PMID:14584941

Abstract

Dimers of vancomycin (Van), linked by a rigid metal complex, Pt(en)(H(2)O)(2), exhibit potent activities (MIC approximately 0.8 mug/mL, approximately 720 times more potent than that of Van itself) against vancomycin-resistant enterococci (VRE). The result suggests that combining metal complexation and receptor/ligand interaction offers a useful method to construct multivalent inhibitors.

摘要

通过刚性金属配合物[Pt(en)(H₂O)₂]²⁺连接的万古霉素（Van）二聚体，对耐万古霉素肠球菌（VRE）表现出强大的活性（最低抑菌浓度约为0.8μg/mL，比Van本身强约720倍）。该结果表明，将金属络合与受体/配体相互作用相结合为构建多价抑制剂提供了一种有用的方法。