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Conjugates of monocyclic β-lactams and siderophore mimetics: a patent evaluation (WO2023023393)
- Source :
- Expert Opinion on Therapeutic Patents; August 2023, Vol. 33 Issue: 7-8 p471-476, 6p
- Publication Year :
- 2023
-
Abstract
- ABSTRACTIntroductionβ-Lactams, which include monobactams, remain the most important class of antibiotics worldwide. Aztreonam, the only monobactam in clinical use, has remarkable activity against many Gram-negative bacteria, but limited activity against some of the most problematic multidrug-resistant (MDR) pathogens, such as MDR Pseudomonas aeruginosaand Acinetobacter baumanniico-expressing extended-spectrum- and metallo-β-lactamases, which can inactivate aztreonam by hydrolysis.Areas coveredStructurally novel siderophore-conjugated aztreonam derivatives with improved antibacterial properties against several high-priority pathogens are claimed. This invention reports that sidechain extension of aztreonam is tolerated; the coupling of its aminothiazoloxime carboxylic acid part with a siderophore mimetic significantly improved the antibacterial activity against several problematic strains, including MDR A. baumanniiisolates with carbapenemase/cephalosporinase activity.Expert OpinionFinding new strategies to tackle bacterial resistance to β-lactam antibiotics is critical. Considering that β lactams are validated and safe drugs, this research may stimulate the field to develop new ideas in the arena of antimicrobial drug discovery, particularly with respect to siderophore mimetics.
Details
- Language :
- English
- ISSN :
- 13543776 and 17447674
- Volume :
- 33
- Issue :
- 7-8
- Database :
- Supplemental Index
- Journal :
- Expert Opinion on Therapeutic Patents
- Publication Type :
- Periodical
- Accession number :
- ejs64440693
- Full Text :
- https://doi.org/10.1080/13543776.2023.2262135