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- Publisher Website: 10.1016/j.bmc.2020.115677
- Scopus: eid_2-s2.0-85088984895
- PMID: 32828420
- WOS: WOS:000562673400002
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Article: Total synthesis and a systematic structure-activity relationship study of WAP-8294A2
Title | Total synthesis and a systematic structure-activity relationship study of WAP-8294A2 |
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Authors | |
Keywords | WAP-8294A2 Total synthesis Alanine scan Lysine scan |
Issue Date | 2020 |
Publisher | Pergamon. The Journal's web site is located at http://www.elsevier.com/locate/bmc |
Citation | Bioorganic & Medicinal Chemistry, 2020, v. 28 n. 18, p. article no. 115677 How to Cite? |
Abstract | WAP-8294A2 is a cyclic peptide antibiotic with novel structure and excellent activity against Gram-positive pathogens. Herein, we report the total synthesis of complex macrocyclic peptide WAP-8294A2 (W1), ent-analogue W2, deoxy analogue W3 and de-methyl analogue W4 using a solid-phase synthetic route followed by a final stage solution-phase cyclization reaction. Exploitation of this process allowed the synthesis of eleven alanine-scanning analogues and eight lysine-scanning analogues. The antimicrobial activity of these analogues was evaluated in vitro against Gram-positive bacteria. Based on the MIC results, a primary systematic structure-activity relationship has been established. |
Persistent Identifier | http://hdl.handle.net/10722/301478 |
ISSN | 2023 Impact Factor: 3.3 2023 SCImago Journal Rankings: 0.614 |
ISI Accession Number ID |
DC Field | Value | Language |
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dc.contributor.author | Chen, D | - |
dc.contributor.author | Tian, L | - |
dc.contributor.author | Po, KHL | - |
dc.contributor.author | Chen, S | - |
dc.contributor.author | Li, X | - |
dc.date.accessioned | 2021-07-27T08:11:41Z | - |
dc.date.available | 2021-07-27T08:11:41Z | - |
dc.date.issued | 2020 | - |
dc.identifier.citation | Bioorganic & Medicinal Chemistry, 2020, v. 28 n. 18, p. article no. 115677 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | http://hdl.handle.net/10722/301478 | - |
dc.description.abstract | WAP-8294A2 is a cyclic peptide antibiotic with novel structure and excellent activity against Gram-positive pathogens. Herein, we report the total synthesis of complex macrocyclic peptide WAP-8294A2 (W1), ent-analogue W2, deoxy analogue W3 and de-methyl analogue W4 using a solid-phase synthetic route followed by a final stage solution-phase cyclization reaction. Exploitation of this process allowed the synthesis of eleven alanine-scanning analogues and eight lysine-scanning analogues. The antimicrobial activity of these analogues was evaluated in vitro against Gram-positive bacteria. Based on the MIC results, a primary systematic structure-activity relationship has been established. | - |
dc.language | eng | - |
dc.publisher | Pergamon. The Journal's web site is located at http://www.elsevier.com/locate/bmc | - |
dc.relation.ispartof | Bioorganic & Medicinal Chemistry | - |
dc.subject | WAP-8294A2 | - |
dc.subject | Total synthesis | - |
dc.subject | Alanine scan | - |
dc.subject | Lysine scan | - |
dc.title | Total synthesis and a systematic structure-activity relationship study of WAP-8294A2 | - |
dc.type | Article | - |
dc.identifier.email | Li, X: xuechenl@hku.hk | - |
dc.identifier.authority | Li, X=rp00742 | - |
dc.description.nature | link_to_subscribed_fulltext | - |
dc.identifier.doi | 10.1016/j.bmc.2020.115677 | - |
dc.identifier.pmid | 32828420 | - |
dc.identifier.scopus | eid_2-s2.0-85088984895 | - |
dc.identifier.hkuros | 323617 | - |
dc.identifier.volume | 28 | - |
dc.identifier.issue | 18 | - |
dc.identifier.spage | article no. 115677 | - |
dc.identifier.epage | article no. 115677 | - |
dc.identifier.isi | WOS:000562673400002 | - |
dc.publisher.place | United Kingdom | - |