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US 2025/0051300 A1Published application
Gram-negative specific antibiotics sparing effect on gut microbiome
AssigneeThe Board of Trustees of the University of Illinois
InventorsPaul J. HERGENROTHER, Kristen A. MUÑOZ
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Abstract
Small molecule inhibitors of the localization of lipoprotein CDE (LolCDE) complex that is found in the membrane of bacteria. Searches for suitable candidates for the LolCDE complex led to the discovery of an inhibitor named lolamycin. Lolamycin specifically targets Gram-negative bacteria such as Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, and Salmonella typhimurium, and is selective over Gram-negative and Gram-positive commensal bacteria, thereby avoiding perturbation of the gut microbiome.
Claims15
A compound of Formula I:
- or a salt thereof;
- wherein
- R1 and R2 are each independently —CH3, —(C2-C6)alkyl or —(C3-C6)cycloalkyl, or H;
- R3 is H, halo, cyano, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl;
- R4 is cyano, H, halo, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl;
- R5 and R6 are each independently H, halo, cyano, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl;
- and
- R7 is H, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl;
- and
- X is O, S, NH, or NCH3;
- wherein any methyl, alkyl, or cycloalkyl moiety is optionally substituted;
- provided that when R1 and R2 are both H, R3 is not F and R3, R4, and R5 are not all H.
9 more elements
Dependencies are inferred from the claim text.