Synthesis and antibacterial studies of teixobactin analogues with non-isostere substitution of enduracididine |
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| Authors: | Kang Jin Kathy Hiu Laam Po Wang Yeuk Kong Chung Hei Lo Chun Wah Lo Ho Yin Lam Amaya Sirinimal Jonathan Avraham Reuven Sheng Chen Xuechen Li |
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| Institution: | 1. Department of Chemistry, State Key Laboratory of Synthetic Chemistry, The University of Hong Kong, Hong Kong Special Administrative Region;2. Department of Applied Biology and Chemical Technology, State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong Special Administrative Region |
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| 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. |
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| Keywords: | Teixobactin analogues Ser ligation SAR study |
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