Synthesis and assessment of bisindoles as a new class of antibacterial agents
| Autor: | Jie Bao, Hua Zhang, Xigong Liu, Shu-Juan Yu, Xue Yan, Ying-De Tang, Fei He |
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| Rok vydání: | 2020 |
| Předmět: |
Indole test
biology Strain (chemistry) 010405 organic chemistry General Chemistry Bacillus subtilis 010402 general chemistry medicine.disease_cause biology.organism_classification 01 natural sciences Combinatorial chemistry 0104 chemical sciences Chiral column chromatography chemistry.chemical_compound chemistry Staphylococcus aureus medicine Enantiomer Growth inhibition Antibacterial activity |
| Zdroj: | Monatshefte für Chemie - Chemical Monthly. 151:971-979 |
| ISSN: | 1434-4475 0026-9247 |
| DOI: | 10.1007/s00706-020-02629-y |
| Popis: | Antimicrobial screening of an in-house library containing both natural products and synthetic compounds identified a bisindole molecule as a selective antibacterial hit. Further evaluation and structural modification afforded a series of dimeric indole derivatives, most of which showed moderate to good antibacterial activity against two Gram-positive strains Staphylococcus aureus and Bacillus subtilis. Chiral HPLC was employed to separate these racemates and the bioactive differences between the enantiomeric pairs were also assessed and discussed. Three dihalogenaged analogues also showed mild growth inhibition against a drug-resistant S. aureus strain. |
| Databáze: | OpenAIRE |
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