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Article: Establishing the Structure–Activity Relationship of Daptomycin

TitleEstablishing the Structure–Activity Relationship of Daptomycin
Authors
KeywordsDaptomycin
Calcium-dependent antibiotics
Structure−activity relationship
Cyclic depsipeptides
Total chemical synthesis
Issue Date2020
PublisherAmerican Chemical Society. The Journal's web site is located at http://pubs.acs.org/toc/amclct/current
Citation
ACS Medicinal Chemistry Letters, 2020, v. 11 n. 7, p. 1442-1449 How to Cite?
AbstractDaptomycin 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.
Persistent Identifierhttp://hdl.handle.net/10722/284532
PubMed Central ID
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorChow, HY-
dc.contributor.authorPo, KHL-
dc.contributor.authorJin, K-
dc.contributor.authorQIAO, G-
dc.contributor.authorSUN, Z-
dc.contributor.authorMA, W-
dc.contributor.authorYe, X-
dc.contributor.authorZhou, N-
dc.contributor.authorChen, S-
dc.contributor.authorLi, XC-
dc.date.accessioned2020-08-07T08:58:59Z-
dc.date.available2020-08-07T08:58:59Z-
dc.date.issued2020-
dc.identifier.citationACS Medicinal Chemistry Letters, 2020, v. 11 n. 7, p. 1442-1449-
dc.identifier.urihttp://hdl.handle.net/10722/284532-
dc.description.abstractDaptomycin 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.-
dc.languageeng-
dc.publisherAmerican Chemical Society. The Journal's web site is located at http://pubs.acs.org/toc/amclct/current-
dc.relation.ispartofACS Medicinal Chemistry Letters-
dc.rightsThis document is the Accepted Manuscript version of a Published Work that appeared in final form in [JournalTitle], copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see [insert ACS Articles on Request author-directed link to Published Work, see http://pubs.acs.org/page/policy/articlesonrequest/index.html].-
dc.subjectDaptomycin-
dc.subjectCalcium-dependent antibiotics-
dc.subjectStructure−activity relationship-
dc.subjectCyclic depsipeptides-
dc.subjectTotal chemical synthesis-
dc.titleEstablishing the Structure–Activity Relationship of Daptomycin-
dc.typeArticle-
dc.identifier.emailChow, HY: hchowhy@connect.hku.hk-
dc.identifier.emailLi, XC: xuechenl@hku.hk-
dc.identifier.authorityLi, XC=rp00742-
dc.description.naturelink_to_OA_fulltext-
dc.identifier.doi10.1021/acsmedchemlett.0c00175-
dc.identifier.pmid32676152-
dc.identifier.pmcidPMC7357220-
dc.identifier.scopuseid_2-s2.0-85088975546-
dc.identifier.hkuros311897-
dc.identifier.volume11-
dc.identifier.issue7-
dc.identifier.spage1442-
dc.identifier.epage1449-
dc.identifier.eissn1948-5875-
dc.identifier.isiWOS:000550767000014-
dc.publisher.placeUnited States-

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