Skip to content
2000
Volume 22, Issue 12
  • ISSN: 1568-0266
  • E-ISSN: 1873-4294

Abstract

Background: Microbial resistance has become a worldwide public health problem and may lead to morbidity and mortality in affected patients. Objectives: Therefore, this work aimed to evaluate the antibacterial activity of quinone-4- oxoquinoline derivatives. Methods: These derivatives were evaluated against Gram-positive and Gram-negative bacteria by their antibacterial activity, anti-biofilm, and hemolytic activities and in silico assays. Results: The quinone-4-oxoquinoline derivatives presented broad-spectrum antibacterial activities and, in some cases, were more active than commercially available reference drugs. These compounds also inhibited bacterial adhesion, and the assays revealed seven non-hemolytic derivatives. The derivatives seem to cause damage to the bacterial cell membrane, and those containing the carboxyl group at the C-3 position of the 4-quinolonic nucleus were more active than those containing a carboxyethyl group. Conclusion: The isoquinoline-5,8-dione nucleus also favored antimicrobial activity. The study showed that the target of the derivatives must be a non-conventional hydrophobic allosteric binding pocket on the DNA gyrase enzyme.

Loading

Article metrics loading...

/content/journals/ctmc/10.2174/1568026622666220504124710
2022-05-01
2025-07-10
Loading full text...

Full text loading...

/content/journals/ctmc/10.2174/1568026622666220504124710
Loading
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test