Antibacterial agents: dual-targeted RNA polymerase inhibitors
AssigneeRutgers, The State University of New Jersey
InventorsRichard H. Ebright, Yon W. Ebright, Chih-Tsung Lin
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Abstract
The invention provides bipartite, dual-targeted inhibitors of bacterial RNA polymerase having the general structural formula (I): X-α-Y (I) wherein X is an moiety that binds to the Rif target of a bacterial RNA polymerase; Y is a moiety that binds to the bridge-helix N-terminus target of a bacterial RNA polymerase; and is a covalent bond or 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.
Claims18
A compound of formula (I):
- X-α-Y (I)
- or a salt thereof, wherein:
- X is selected from rifamycin, streptovaricin, tolypomycin, or sorangicin;
- Y is selected from a CBR hydrazide, a CBR pyrazole, or an Nα-aroyl-N-aryl-phenylalaninamide;
- and
- α is a covalent bond or a linker.
A compound, or a salt thereof, selected from:
- or a tautomer or salt thereof.
The compound,
- or a salt thereof.
Dependencies are inferred from the claim text.