Synthesis and antibacterial studies of teixobactin analogues with non-isostere substitution of enduracididine

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

21 Scopus Citations
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Author(s)

  • Kang Jin
  • Kathy Hiu Laam Po
  • Wang Yeuk Kong
  • Chung Hei Lo
  • Chun Wah Lo
  • Ho Yin Lam
  • Amaya Sirinimal
  • Jonathan Avraham Reuven
  • Xuechen Li

Detail(s)

Original languageEnglish
Pages (from-to)1062-1068
Journal / PublicationBioorganic and Medicinal Chemistry
Volume26
Issue number5
Online published1 Feb 2018
Publication statusPublished - 1 Mar 2018
Externally publishedYes

Abstract

Teixobactin is a structurally and mechanistically novel antimicrobial peptide with potent activities against Gram-positive pathogens. It contains L-allo-enduracididine (End) residue which is not readily accessible. In this report, we have used convergent Ser Ligation as the key step to prepare a series of teixobactin analogues with End being substituted with its non-isostere moieties. Among these analogues, compounds T16, T27 and T29 exhibited the best antimicrobial activities against different Gram-positive bacteria with MICs ranging from 0.25 to 1.0 µM. Structure-activity relationship is also established for further development of more promising teixobactin analogues.

Research Area(s)

  • SAR study, Ser ligation, Teixobactin analogues

Citation Format(s)

Synthesis and antibacterial studies of teixobactin analogues with non-isostere substitution of enduracididine. / Jin, Kang; Po, Kathy Hiu Laam; Kong, Wang Yeuk; Lo, Chung Hei; Lo, Chun Wah; Lam, Ho Yin; Sirinimal, Amaya; Reuven, Jonathan Avraham; Chen, Sheng; Li, Xuechen.

In: Bioorganic and Medicinal Chemistry, Vol. 26, No. 5, 01.03.2018, p. 1062-1068.

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