Abstract
Synthesis was achieved via reactions between a variety of indole-7-carbaldehydes and rhodanine, N-allylrhodanine, barbituric acid or thiobarbituric acid. A library of structurally diverse compounds was examined by enzyme-linked immunosorbent assay (ELISA) to assess the inhibition of the targeted protein–protein interaction. Inhibition of bacterial growth was also evaluated using Bacillus subtilis and Escherichia coli cultures. The structure–activity relationship studies demonstrated the significance of particular structural features of the synthesized molecules for RNA polymerase-σ70/σAinteraction inhibition and antibacterial activity. Docking was investigated as an in silico method for the further development of the compounds.
Original language | English |
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Pages (from-to) | 4302-4308 |
Number of pages | 7 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 27 |
Issue number | 18 |
DOIs | |
Publication status | Published - 1 Jan 2017 |
Keywords
- Antibacterial activity
- Bacterial transcription
- Indole
- RNA polymerase
- Structure-activity relationship (SAR)
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry