Small molecule inhibitors of bacterial transcription complex formation

Daniel S. Wenholz, Ming Zeng, Cong Ma, Marcin Mielczarek, Xiao Yang, Mohan Bhadbhade, David St C. Black, Peter J. Lewis, Renate Griffith, Naresh Kumar

Research output: Journal article publicationJournal articleAcademic researchpeer-review

8 Citations (Scopus)

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 languageEnglish
Pages (from-to)4302-4308
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number18
DOIs
Publication statusPublished - 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

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