Novel class of antibiotics effective against drug-resistant bacteria

Unmet Need

Antimicrobial resistance among Gram-negative bacilli is increasing and becoming alarmingly common, especially as bacterial strains become resistant to multiple antibiotics. The infectious diseases caused by multidrug-resistant bacteria pose serious threats to humankind. There clearly is an urgent need for new antibiotics, particularly those with novel mechanisms of action. The gene LpxC encodes the enzyme that is involved in the synthesis of lipid A which is an essential component of all Gram-negative bacteria. Inhibiting the enzymatic activity of LpxC would help to defeat the resistance mechanisms. Scientists first suggested targeting LpxC as a treatment strategy more than 20 years ago, but researchers have been unable to identify a compound that was safe at effective dosage levels.

Technology

Duke researchers have synthesized novel antibiotics that inhibit LpxC, an essential enzyme of the lipid A biosynthetic pathway in Gram-negative bacteria. Being LpxC inhibitors they target a pathway that has never been exploited by current antibiotics, and therefore they should be very effective for multidrug-resistant strains of bacteria. These components have been shown to be effective in vitro against a broad panel of Gram-negative clinical isolates, including several multiresistant and extremely drug-resistant strains involved in nosocomial infections.

Advantages

  • Have potential for clinical development as therapeutics for infections caused by multidrug-resistant bacteria
  • A new class of antibiotics against fatal infections caused by extremely virulent pathogens.
  • Safe and efficient
Artistic rendering of bacteria with blue background

Duke File (IDF) Number

T-004143

Inventor(s)

  • Zhou, Pei
  • GopalaSwamy, Ramesh
  • Lee, Chuljin
  • Liang, Xiaofei
  • Toone, Eric

Patents

    • Patent Number: 10,647,664
    • Title: SUBSTITUTED HYDROXAMIC ACID COMPOUNDS
    • Country: United States of America
    • Patent Number: 10,647,664
    • Title: SUBSTITUTED HYDROXAMIC ACID COMPOUNDS
    • Country: United States of America
    • Patent Number: 10,189,786
    • Title: ANTIBACTERIAL COMPOUNDS
    • Country: United States of America
    • Patent Number: 10,189,786
    • Title: ANTIBACTERIAL COMPOUNDS
    • Country: United States of America
    • Patent Number: 9,908,851
    • Title: 2-PIPERIDINYL SUBSTITUTED N,3-DIHYDROXYBUTANAMIDES
    • Country: United States of America
    • Patent Number: 9,908,851
    • Title: 2-PIPERIDINYL SUBSTITUTED N,3-DIHYDROXYBUTANAMIDES
    • Country: United States of America
    • Patent Number: 6458270
    • Title: SUBSTITUTED HYDROXAMIC ACID COMPOUNDS
    • Country: Japan
    • Patent Number: 6458270
    • Title: SUBSTITUTED HYDROXAMIC ACID COMPOUNDS
    • Country: Japan

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College

School of Medicine (SOM)