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Synthesis and Antibacterial Activity of New 6″-Modified Tobramycin Derivatives.
Antibiotics (Basel)
December 2024
Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow 119021, Russia.
Aminoglycosides are one of the first classes of natural antibiotics which have not lost relevance due to their broad spectrum of action against Gram-positive, Gram-negative bacteria and mycobacteria. The high growth rate of antimicrobial resistance (AMR) together with the severe side effects of aminoglycosides increase the importance of developing improved semisynthetic derivatives. In this work, we proposed a synthetic route to new tobramycin derivatives modified at the 6″-position with aminoalkylamine or guanidinoalkylamine residues.
View Article and Find Full Text PDFSoloxolone -3-(Dimethylamino)propylamide Restores Drug Sensitivity of Tumor Cells with Multidrug-Resistant Phenotype via Inhibition of P-Glycoprotein Efflux Function.
Molecules
October 2024
Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
Article Synopsis
- Multidrug resistance (MDR) in cancer therapy is largely due to the overexpression of P-glycoprotein (P-gp), prompting the need for effective P-gp inhibitors to enhance drug efficacy.
- The study verified the P-gp inhibitory and MDR reversing activities of soloxolone amides, which showed significant binding capability to P-gp, and enhanced the uptake of drugs like Rhodamine 123 and doxorubicin in cancer cell lines.
- The results indicate that one specific soloxolone amide not only outperformed the established inhibitor verapamil in some cases but also showed potential as a drug candidate for overcoming P-gp-mediated MDR in tumor cells.
Probing amikacin interaction with albumin: A combined multispectral and molecular docking investigation.
Heliyon
October 2024
Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
The fate of a drug administered to a living organism depends on the pharmacological and pharmacokinetic behavior of drugs. Biological macromolecules like serum albumins have a crucial role in the design and biological safety assessments of drugs. Amikacin as an example of the most used semi-synthetic aminoglycosides antibiotics, is included in the crucial drug list of the World Health Organization.
View Article and Find Full Text PDFSpectinamide MBX-4888A exhibits favorable lesion and tissue distribution and promotes treatment shortening in advanced murine models of tuberculosis.
Antimicrob Agents Chemother
November 2024
Department of Microbiology, Immunology and Pathology, Mycobacteria Research Laboratories, Colorado State University, Fort Collins, Colorado, USA.
Article Synopsis
- Scientists created new medicines called spectinamides to help treat tuberculosis (TB) more effectively.
- One of these, named MBX-4888A, works well with other TB drugs like rifampin and pyrazinamide in mice.
- The research showed that using MBX-4888A can help shorten the treatment time for TB and seems to be safe for long-term use in mice.
Glycodiversification of gentamicins through glycosyltransferase swapping enabled the creation of novel hybrid aminoglycoside antibiotics with potent activity and low ototoxicity.
Acta Pharm Sin B
September 2024
Department of Hematology, Zhongnan Hospital of Wuhan University, School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.
Aminoglycosides (AGs) are a class of antibiotics with a broad spectrum of activity. However, their use is limited by safety concerns associated with nephrotoxicity and ototoxicity, as well as drug resistance. To address these issues, semi-synthetic approaches for modifying natural AGs have generated new generations of AGs, however, with limited types of modification due to significant challenges in synthesis.
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