Novel pleuromutilin derivatives conjugated with phenyl-sulfide and boron-containing moieties as potent antibacterial agents against antibiotic-resistant bacteria.
Eur J Med Chem
; 277: 116745, 2024 Nov 05.
Article
in En
| MEDLINE
| ID: mdl-39106659
ABSTRACT
In response to the escalating threat of microbial resistance, a series of novel pleuromutilin derivatives, conjugated with phenyl-sulfide and boron-containing moieties, were designed and synthesized. Most derivatives, especially 14b and 16b, demonstrated significant efficacy against Gram-positive bacteria, including multidrug-resistant strains, as well as pleuromutilin-resistant strains. Compound 16b showed high stability in the liver microsomes of rats and humans, along with acceptable tolerance in vitro and in vivo. Additionally, compound 16b exhibited promising efficacy in MRSA-infected mouse models. Our data highlight the potential of conjugated pleuromutilin derivatives as valuable agents against drug-resistant bacteria.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Polycyclic Compounds
/
Microbial Sensitivity Tests
/
Diterpenes
/
Pleuromutilins
/
Anti-Bacterial Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Eur J Med Chem
Year:
2024
Document type:
Article
Affiliation country:
China
Country of publication:
France