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

TitleSynthesis and antibacterial studies of teixobactin analogues with non-isostere substitution of enduracididine
Authors
Issue Date2018
PublisherPergamon. The Journal's web site is located at http://www.elsevier.com/locate/bmc
Citation
Bioorganic & Medicinal Chemistry, 2018, v. 26 n. 5, p. 1062-1068 How to Cite?
AbstractTeixobactin 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.
Persistent Identifierhttp://hdl.handle.net/10722/256266
ISSN
2019 Impact Factor: 3.073
2015 SCImago Journal Rankings: 1.064
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorJin, K-
dc.contributor.authorPo, KHL-
dc.contributor.authorKong, WY-
dc.contributor.authorLo, CH-
dc.contributor.authorLo, CW-
dc.contributor.authorLam, HY-
dc.contributor.authorSirinimal, A-
dc.contributor.authorReuven, JA-
dc.contributor.authorChen, S-
dc.contributor.authorLi, XC-
dc.date.accessioned2018-07-20T06:31:56Z-
dc.date.available2018-07-20T06:31:56Z-
dc.date.issued2018-
dc.identifier.citationBioorganic & Medicinal Chemistry, 2018, v. 26 n. 5, p. 1062-1068-
dc.identifier.issn0968-0896-
dc.identifier.urihttp://hdl.handle.net/10722/256266-
dc.description.abstractTeixobactin 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.-
dc.languageeng-
dc.publisherPergamon. The Journal's web site is located at http://www.elsevier.com/locate/bmc-
dc.relation.ispartofBioorganic & Medicinal Chemistry-
dc.rightsThis work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.-
dc.titleSynthesis and antibacterial studies of teixobactin analogues with non-isostere substitution of enduracididine-
dc.typeArticle-
dc.identifier.emailLi, XC: xuechenl@hku.hk-
dc.identifier.authorityLi, XC=rp00742-
dc.description.naturepostprint-
dc.identifier.doi10.1016/j.bmc.2018.01.016-
dc.identifier.hkuros286398-
dc.identifier.volume26-
dc.identifier.issue5-
dc.identifier.spage1062-
dc.identifier.epage1068-
dc.identifier.isiWOS:000425552300008-
dc.publisher.placeUnited Kingdom-

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