| 2 min read
Register for free to listen to this article
Listen with Speechify
0:00
2:00
WEST LAFAYETTE, Ind.—Clostridioides difficile, also known as C. diff, is a leading cause of health care-associated infection in the U.S. Two antibiotics, vancomycin and fidaxomicin, are approved by the U.S. Food and Drug Administration for the treatment of C. diff, but even these therapies suffer from high treatment failure and recurrence.
 
Purdue University researchers have advanced novel compounds they developed to help treat patients with C. diff, which is one of four bacteria considered an urgent threat by the Centers for Disease Control and Prevention. Their work was published in an article in the Journal of Medicinal Chemistry.
 
“Our compounds have several advantages, including ultrapotent activities with minimum inhibitory concentration values as low as 0.003 μg/mL,” said Herman O. Sintim, the Drug Discovery Professor of Chemistry at Purdue University. “Our compounds also do not kill good bacteria at concentrations that kill C. diff and performed significantly better than current antibiotics in preventing recurrence. These are significant advantages for patients dealing with this difficult bacterial infection.”
 
“Trifluoromethylthio containing N-(1,3,4-oxadiazol-2-yl) benzamides displayed very potent activities (sub-µg/mL minimum inhibitory concentration (MIC) values) against Gram-positive bacteria,” notes the article abstract. “Here, we report remarkable antibacterial activity enhancement via halogen substitutions, which afford new anti-C. difficile agents with ultrapotent activities (MICs as low as 0.003 µg/mL (0.007 µM)) that surpassed the activity of vancomycin against C. difficile clinical isolates.”
 
“The most promising compound in the series, HSGN-218, was non-toxic to mammalian colon cells and is gut restrictive. In addition, HSGN-218 protected mice from CDI [C. difficile infections] recurrence,” the article continues. “Not only does this work provide a potential clinical lead for the development of C. difficile therapeutics but also it highlights dramatic drug potency enhancement via halogen substitution.”
 
Sintim pointed out that HSGN-218 has been shown to be one of the most potent compounds ever produced for use against C. diff.
 
“This is part of our work to create new solutions to treat diseases and infections, which are resistant to current treatment options,” added Sintim, who is also a member of the Purdue University Center for Cancer Research and the Purdue Institute for Drug Discovery. “This work provides a potential clinical lead for the development of C. diff therapeutics and also highlights dramatic drug potency enhancement via halogen substitution.”

About the Author

Related Topics

Loading Next Article...
Loading Next Article...
Subscribe to Newsletter

Subscribe to our eNewsletters

Stay connected with all of the latest from Drug Discovery News.

Subscribe

Sponsored

Gold circles with attached purple corkscrew shapes represent gold nanoparticles against a black background.

Driving gene therapy with nonviral vectors 

Learn why nonviral vectors are on the rise in gene therapy development.
A 3D digital illustration of a viral spike protein on a cell surface, surrounded by colorful, floating antibodies in the background

Milestone: Leapfrogging to quantitative, high throughput protein detection and analysis

Researchers continuously push the boundaries of what’s possible with protein analysis tools.
Blue cancer cells attached to a cellular surface against a bright blue background in a 3D rendering of a cancer infection.

Advancing immuno-oncology research with cellular assays

Explore critical insights into immunogenicity and immunotoxicity assays for cancer therapies.
Drug Discovery News November 2024 Issue
Latest IssueVolume 20 • Issue 6 • November 2024

November 2024

November 2024 Issue

Explore this issue