Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/75884
Title: Small molecule inhibitors of bacterial transcription complex formation
Authors: Wenholz, DS
Zeng, M
Ma, C 
Mielczarek, M
Yang, X 
Bhadbhade, M
Black, DS
Lewis, PJ
Griffith, R
Kumar, N
Keywords: Antibacterial activity
Bacterial transcription
RNA polymerase
Structure-activity relationship (SAR)
Indole
Issue Date: 2017
Publisher: Pergamon Press
Source: Bioorganic & medicinal chemistry letters, 2017, v. 27, no. 18, p. 4302-4308 How to cite?
Journal: Bioorganic & medicinal chemistry letters 
Abstract: Knoevenagel condensation was employed to generate a set of molecules potentially capable of inhibiting the RNA polymerase-sigma(70)/sigma(A) 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-sigma(70)/sigma(A) interaction inhibition and antibacterial activity. Docking was investigated as an in silico method for the further development of the compounds.
URI: http://hdl.handle.net/10397/75884
ISSN: 0960-894X
EISSN: 1464-3405
DOI: 10.1016/j.bmcl.2017.08.036
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