Rui Liu

Title: Innovations by Inventor Rui Liu

Introduction

Rui Liu is a notable inventor based in South Bend, IN (US). He has made significant contributions to the field of antimicrobial compounds, holding 2 patents that showcase his innovative work. His research focuses on developing new antibiotics that can combat resistant strains of bacteria.

Latest Patents

One of Rui Liu's latest patents involves deuterated antimicrobial compounds. Substituted nitrobenzothiazinones (BTZs) are identified as potent antituberculosis prodrugs that are reductively activated to produce nitroso moieties. These moieties form covalent adducts with a cysteine residue of decaprenylphosphoryl-β-D-ribose-2'-oxidase (DprE1) of Mycobacterium tuberculosis (Mtb). The resulting inhibition of cell wall synthesis is lethal to Mtb, leading to the consideration of BTZs for clinical use. The hydride-induced reduction of the nitroaromatic proceeds by reversible formation of the corresponding Meisenheimer complex. Liu demonstrates that chemical reduction of BTZ043 with NaBD4 followed by reoxidation incorporates deuterium into the core nitro aromatic warhead. This process prolongs the lifetime of the active nitroso oxidation state due to the deuterium isotope effect.

Another significant patent by Liu focuses on antibacterial monobactams. Bromine-induced lactamization of vinyl acetohydroxamates facilitates the synthesis of monocyclic β-lactams suitable for incorporating a thiomethyl and extended functionality at the C(4) position. The elaboration of the resulting substituted N-hydroxy-2-azetidinones allows for the incorporation of functionalized α-amino substituents, enhancing antibiotic activity. Evaluation of antibacterial activity against a panel of Gram-positive and Gram-negative bacteria revealed structure-activity relationships (SAR) and identified potent new monobactam antibiotics. The corresponding bis-catechol conjugate has shown excellent activity against Gram-negative bacteria, including strains producing carbapenemase and carbacephalosporinase, which are listed by the WHO as critical concerns worldwide.

Career Highlights

Rui Liu is affiliated with the University of Notre Dame Du Lac, where he continues to advance his research in antimicrobial compounds. His work has garnered attention for its potential impact on public health, particularly