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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Chen D,Tian L,Po KHL,Chen S,Li Xdoi
10.1016/j.bmc.2020.115677subject
Has Abstractpub_date
2020-09-15 00:00:00pages
115677issue
18eissn
0968-0896issn
1464-3391pii
S0968-0896(20)30507-1journal_volume
28pub_type
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