Bipartite inhibitors of bacterial RNA polymerase

US9415112B2 · kind B2 · utility

Assignee

• Rutgers, the State University of New Jersey · US

Inventors

• Richard H. Ebright · New Brunswick, US
• David Degen · New Brunswick, US
• Yu Zhang · Shanghai, CN
• Yon W. Ebright · New Brunswick, US

Key dates

• Filing date: Jun 20, 2012
• Grant date: Aug 16, 2016
• Expiry date: Jun 20, 2032

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention provides bipartite inhibitors of bacterial RNA polymerase having the general structural formula (I): X-α-Y (I) wherein X is an moiety that binds to the rifamycin binding site of a bacterial RNA polymerase, Y is a moiety that binds to the GE23077 binding site of a bacterial RNA polymerase, and is a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.