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Total synthesis and a systematic structure-activity relationship study of WAP-8294A2.
- Source :
-
Bioorganic & Medicinal Chemistry . Sep2020, Vol. 28 Issue 18, pN.PAG-N.PAG. 1p. - Publication Year :
- 2020
-
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 (W 1) , ent -analogue W 2 , deoxy analogue W 3 and de-methyl analogue W 4 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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 09680896
- Volume :
- 28
- Issue :
- 18
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 145440712
- Full Text :
- https://doi.org/10.1016/j.bmc.2020.115677