Establishing the Structure−Activity Relationship of Daptomycin

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal

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Author(s)

  • Hoi Yee Chow
  • Kathy Hiu Laam Po
  • Kang Jin
  • Guanlin Qiao
  • Zhenquan Sun
  • Wenjie Ma
  • Xiyun Ye
  • Ning Zhou
  • Xuechen Li

Detail(s)

Original languageEnglish
Pages (from-to)1442-1449
Number of pages8
Journal / PublicationACS Medicinal Chemistry Letters
Volume11
Issue number7
Online published3 Jun 2020
Publication statusPublished - 9 Jul 2020

Abstract

Daptomycin is effective in treating infections caused by antibiotic-resistant Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococci (VRE), and vancomycin-resistant S. aureus (VRSA). Due to its distinct mechanism of action toward multidrug-resistant bacteria, daptomycin provides an attractive structural motif to generate new daptomycin-based antibiotics to combat the problem of bacterial resistance. In this study, we used the total synthesis method to produce daptomycin analogues with a variety in terms of types and sites of modifications. Five classes of daptomycin analogues were synthesized, and the antimicrobial activities of the analogues were analyzed by several biological assays. From this study, we established a comprehensive structure−activity relationship of daptomycin which will lay the foundation for the further development of daptomycin-based antibiotics. Copyright © 2020 American Chemical Society.

Research Area(s)

  • Calcium-dependent antibiotics, Cyclic depsipeptides, Daptomycin, Structure−activity relationship, Total chemical synthesis

Citation Format(s)

Establishing the Structure−Activity Relationship of Daptomycin. / Chow, Hoi Yee; Po, Kathy Hiu Laam; Jin, Kang; Qiao, Guanlin; Sun, Zhenquan; Ma, Wenjie; Ye, Xiyun; Zhou, Ning; Chen, Sheng; Li, Xuechen.

In: ACS Medicinal Chemistry Letters, Vol. 11, No. 7, 09.07.2020, p. 1442-1449.

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal