- Title
- Small molecule inhibitors of bacterial transcription complex formation
- Creator
- Wenholz, Daniel S.; Zeng, Ming; Ma, Cong; Mielczarek, Marcin; Yang, Xiao; Bhadbhade, Mohan; Black, David St. C.; Lewis, Peter J.; Griffith, Renate; Kumar, Naresh
- Relation
- NHMRC.1008014 http://purl.org/au-research/grants/nhmrc/1008014
- Relation
- Bioorganic and Medicinal Chemistry Letters Vol. 27, Issue 18, p. 4302-4308
- Publisher Link
- http://dx.doi.org/10.1016/j.bmcl.2017.08.036
- Publisher
- Elsevier
- Resource Type
- journal article
- Date
- 2017
- Description
- Knoevenagel condensation was employed to generate a set of molecules potentially capable of inhibiting the RNA polymerase-σ70/σA interaction in bacteria. 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/σA interaction inhibition and antibacterial activity. Docking was investigated as an in silico method for the further development of the compounds.
- Subject
- antibacterial activity; bacterial transcription; RNA polymerase; structure-activity relationship (SAR); indole
- Identifier
- http://hdl.handle.net/1959.13/1350468
- Identifier
- uon:30559
- Identifier
- ISSN:0960-894X
- Language
- eng
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