Bacterial DNA gyrase inhibitors and methods of use thereof
AssigneesThe Florida International University Board of Trustees, University of Central Florida Research Foundation, Inc.
InventorsFenfei Leng, Eddy Alfonso, Zifang Deng, Adel Nefzi, Kyle Rohde
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Abstract
The subject invention provides fluorophore-quencher nucleic acid molecules comprising relaxed or supercoiled DNA molecules, and their use in rapid and efficient high-throughput screening (HTS) assays to screen and identify compounds that inhibit DNA gyrases. These compounds can be used as antibiotics for treating bacterial infections, especially, multidrug resistant bacterial infections.
Claims15
A method for inhibiting a DNA gyrase, comprising contacting the DNA gyrase with a compound having a structure of formula (V):
- wherein X is selected from CH, CR and N;
- R, R10 and R12 are each independently selected from halogen, hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, substituted alkenyl, alkynyl, haloalkyl, acyl, substituted acyl, alkoxyl, hydroxyl, carboxyl, carbonyl, amine, amide, ester, haloalkyl, haloaryl, thiol, thioamide, urea, and thiourea;
- and R11 is selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl substituted alkenyl, alkynyl, haloalkyl, acyl, substituted acyl, alkoxyl, hydroxyl, carboxyl, carbonyl, amine, amide, ester, haloalkyl, haloaryl, thiol, thioamide, urea, and thiourea.
A method for treating a bacterial infection in a subject, the method comprising administering to the subject in need of such treatment a pharmaceutical composition comprising a compound having a general structure of:
- of formula (V)
- wherein X is selected from CH, CR and N;
- R, R10 and R12 are each independently selected from halogen, hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, substituted alkenyl, alkynyl, haloalkyl, acyl, substituted acyl, alkoxyl, hydroxyl, carboxyl, carbonyl, amine, amide, ester, haloalkyl, haloaryl, thiol thioamide, urea, and thiourea;
- and R11 is selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl substituted alkenyl, alkynyl, haloalkyl, acyl, substituted acyl, alkoxyl, hydroxyl, carboxyl, carbonyl, amine, amide, ester, haloalkyl, haloaryl, thiol, thioamide, urea, and thiourea.
Dependencies are inferred from the claim text.