Following the preparation of an inclusion complex of β-cyclodextrin and meropenem, methods based on FT-IR, Raman and DSC were used for its characterization. An analysis of changes in the stability of meropenem after complexation showed that the complex may serve as a valuable delivery system significantly contributing to enhanced meropenem stability in aqueous solutions and in the solid phase. Due to a sustained transfer of meropenem from the cavity of the cyclodextrin it was possible to maintain a constant desired meropenem concentration over a period of 20 h, as confirmed by a release study. An evaluation of microbial activity not only demonstrated that the bactericidal action of meropenem was not stopped as a result of complexation but even pointed to greater growth inhibition in certain clinically important strains. The fact that investigations of meropenem stability and microbial activity proposed the carbonyl groups as those domains of a meropenem molecule that are instrumental in the formation of a complex with β-cyclodextrin supports the findings of theoretical studies based on molecular modeling.
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http://dx.doi.org/10.1016/j.ejpb.2015.10.013 | DOI Listing |
Cell Mol Biol (Noisy-le-grand)
January 2025
Laboratory of Plant Improvement and Valorization of Agro-resources, National School of Engineers of Sfax, University of Sfax, Sfax LR.16ES20, Tunisia.
Urinary tract infections (UTIs) are recognized as the second most common medical condition, following respiratory infections. Despite the availability of numerous efficacious antibiotics for the management of UTIs, the rising incidence of bacterial resistance presents significant challenges in the treatment of these infections. Bacteria are endowed with the ability to reproduce and develop resistance mechanisms against antibiotics.
View Article and Find Full Text PDFEur J Med Chem
January 2025
Laboratory for Marine Drugs and Bioproducts, Qingdao Marine Science and Technology Center, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266071, China. Electronic address:
The emergence of New Delhi metallo-β-lactamase-1 (NDM-1) poses a significant threat to the clinical application of antibiotics, as it possesses the ability to hydrolyze nearly all β-lactam antibiotics. Regrettably, there are currently no clinical drugs targeting NDM-1, making it imperative to develop highly potent and minimally toxic NDM-1 inhibitors. Herein, a series of molecular Trojan horses targeting NDM-1 were synthesized by introducing ebselen into 7-aminocephalosporanic acid derivatives via a C-Se bond.
View Article and Find Full Text PDFAntimicrob Agents Chemother
January 2025
Microbiology department, A Coruna University Hospital (CHUAC), Institute of Biomedical Research of A Coruna (INIBIC), A Coruna, Spain.
Carbapenemase OXA-48 and its variants pose a serious threat to the development of effective treatments for bacterial infections. OXA-48-producing Enterobacterales are the most prevalent carbapenemase-producing bacteria in large parts of the world. Although these bacteria exhibit low-level carbapenem resistance , the infections they cause are challenging to treat with conventional therapies, owing to their spread and complex detection in clinical settings.
View Article and Find Full Text PDFJ Pediatric Infect Dis Soc
January 2025
IHMA, Schaumburg, IL, USA.
Objectives: To evaluate the in vitro susceptibility of recent Gram-negative pathogens collected from pediatric patients to imipenem/relebactam (IMI/REL) and comparator agents.
Methods: From 2018 to 2022, 254 hospitals in 62 countries collected Enterobacterales or P. aeruginosa isolates from patients <18 years old as part of the SMART global surveillance program.
J Glob Antimicrob Resist
January 2025
Department of Public Health and Infectious Diseases, Sapienza University of Rome, Rome, Italy. Electronic address:
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