Rational design and synthesis of non-competitive transcription inhibitors targeting a conserved RNA polymerase-σ A interface

Key Points

• The aim is to design and synthesize transcription inhibitors that target a specific interface of RNA polymerase-σ A.
• Conducted in silico screening to identify potential transcription inhibitors.
• Designed non-competitive inhibitors targeting RNA polymerase-σ A interface.
• Synthesized selected inhibitors based on screening results.
• Identified novel M. tuberculosis transcription inhibitors with bactericidal properties.
• Demonstrated efficacy of inhibitors through in vitro assays.