Synthesis and antifungal activities of cyclic octa-lipopeptide burkholdine analogues
| Autor: | Hiroyuki Konno, Kazuto Nosaka, Kenta Matsuzaki, Yusuke Otsuki |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Antifungal Agents
Stereochemistry Candida viswanathii Aspergillus oryzae Clinical Biochemistry Pharmaceutical Science Stereoisomerism Microbial Sensitivity Tests Saccharomyces cerevisiae Biochemistry Peptides Cyclic chemistry.chemical_compound Lipopeptides Structure-Activity Relationship Drug Discovery Side chain Structure–activity relationship Amino Acid Sequence Molecular Biology Peptide sequence Candida chemistry.chemical_classification biology Organic Chemistry Lipopeptide biology.organism_classification Amino acid chemistry Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry letters. 23(14) |
| ISSN: | 1464-3405 |
| Popis: | Synthesis and antifungal activity of cyclic octapeptide derivatives of burkholdines are described. To construct cyclic octapeptides, the combination of Fmoc-SPPS and cyclization with DIC/HOBt in the solution phase was employed. Synthesized peptides were evaluated for antifungal activity with MIC values against Saccharomyces cerevisiae, Aspergillus oryzae, and Candida viswanathii. As a result, the lipid side chain and the stereochemistry of each amino acid of Bk-1097 analogues significantly affected antifungal activity. |
| Databáze: | OpenAIRE |
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