COMPOUNDS FOR TREATMENT OF FLUOROQUINOLONE-RESISTANT BACTERIA

摘要

Compounds that specifically kill fluoroquinolone (FQ) resistant bacteria have been developed and are described herein. The FQs are the most commonly prescribed antibiotics to adults in the U.S. and thus are extremely important drugs. However, bacterial resistant to these drugs is now ubiquitous in some of the most common and deadly Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Indeed, FQs are no longer indicated for treatment of MRSA and VRE infections because of such resistance. The compounds have specific and potent activity versus MRSA and VRE.

主权项

1. A compound of Formula I:wherein
R1 is (C1-C12)alkyl, (C1-C12)alkyl(C3-C12)cycloalkyl, or (C3-C12)cycloalkyl, where alkyl can be straight or branched; R2 is (C1-C12)alkyl, (C1-C12)alkyl(C3-C12)cycloalkyl, or (C3-C12)cycloalkyl, where alkyl can be straight or branched; R3 is (C1-C12)alkyl, (C1-C12)alkyl(C3-C12)cycloalkyl, or (C3-C12)cycloalkyl, where alkyl can be straight or branched; and R4 is H, (C1-C12)alkyl, (C1-C12)alkyl(C3-C12)cycloalkyl, or (C3-C12)cycloalkyl, where alkyl can be straight or branched; provided that when R4 is H, R1, R2, and R3 are not each methyl.