Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 46, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2021.116343
Keywords
beta-lactam antibiotic; Tricyclic beta-lactam; gamma-lactone; Sulfoxide; Carbapenem-resistant Enterobacterale; beta-lactamase
Ask authors/readers for more resources
A series of tricyclic beta-lactams were synthesized and evaluated for antibacterial activities against carbapenem-resistant Enterobacterales (CBEs). Introducing sulfoxide resulted in potent antibacterial activities and strong therapeutic efficacy in a neutropenic mouse lung infection model. The tricyclic beta-lactam skeleton may serve as a promising scaffold for new antibacterial agents against CREs.
A series of tricyclic beta-lactams were synthesized and evaluated for in vitro antibacterial activities against carbapenem-resistant Enterobacterales (CBEs). Starting from a reported tricyclic beta-lactam that combined the cephalosporin skeleton having a gamma-lactone ring with a carboxylic acid group, which was reported as a unique partial structure of Lactivicin, we identified the compound which shows potent antibacterial activities against all tested CREs by introducing sulfoxide. In addition, the sulfoxide-introduced tricyclic beta-lactam also shows a strong therapeutic efficacy in the neutmpenic mouse lung infection model. These results indicate that the tricyclic beta-lactam skeleton will show sufficient therapeutic performance in clinical use and therefore can serve as a scaffold in the search for new antibacterial agents against CREs.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available