The synthesis and in vitro activity of 7 beta-[(Z)-2-(2-amino-4-thiazolyl)-2-(2-carboxy-2- alkoxyimino)acetamido]cephalosporins with a (4-carboxy-3-hydroxy-5-isothiazolyl)thiomethyl group at the 3-position are described. These cephalosporins (9a approximately 9i) showed excellent activity against Gram-negative bacteria including beta-lactamase producing strains. The most interesting compound of the series was 7 beta-[(Z)-2-(2-amino-4-thiazolyl)-2- (2-carboxy-2-propoxyimino)acetamido]-3-cephem-4-carboxylic acid (9g, YM-13115) because of its outstanding inhibitory potency against Pseudomonas aeruginosa and highly prolonged plasma half-life in rats.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.7164/antibiotics.40.173 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Clinical and mechanistic insights into biomedical application of Se-enriched probiotics and biogenic selenium nanoparticles.
Biotechnol Lett
January 2025
Extremophile and Productive Microorganisms Research Center, Kerman University of Medical Sciences, Kerman, Iran.
Selenium is an essential element with various industrial and medical applications, hence the current considerable attention towards the genesis and utilization of SeNPs. SeNPs and other nanoparticles could be achieved via physical and chemical methods, but these methods would not only require expensive equipment and specific reagents but are also not always environment friendly. Biogenesis of SeNPs could therefore be considered as a less troublesome alternative, which opens an excellent window to the selenium and nanoparticles' world.
View Article and Find Full Text PDFDefective Mammary Epithelial Outgrowth in Transgenic EKAREV-NLS Mice: Correction via Estrogen Supplementation and Genetic Background Modification.
J Mammary Gland Biol Neoplasia
January 2025
Department of Histology and Embryology, Faculty of Medicine, Masaryk University, Brno, Czech Republic.
Fluorescent biosensors offer a powerful tool for tracking and quantifying protein activity in living systems with high temporospatial resolution. However, the expression of genetically encoded fluorescent proteins can interfere with endogenous signaling pathways, potentially leading to developmental and physiological abnormalities. The EKAREV-NLS mouse model, which carries a FRET-based biosensor for monitoring extracellular signal-regulated kinase (ERK) activity, has been widely utilized both in vivo and in vitro across various cell types and organs.
View Article and Find Full Text PDFDesign, synthesis, and in vitro antitumor evaluation of novel benzimidazole acylhydrazone derivatives.
Mol Divers
January 2025
State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang, Guizhou, 550025, People's Republic of China.
This study focuses on the design, synthesis, and evaluation of benzimidazole derivatives for their anti-tumor activity against A549 and PC-3 cells. Initial screening using the MTT assay identified compound 5m as the most potent inhibitor of A549 cells with an IC of 7.19 μM, which was superior to the positive agents 5-Fluorouracil and Gefitinib.
View Article and Find Full Text PDFADAR1 Promotes the Progression and Temozolomide Resistance of Glioma Through p62-Mediated Selective Autophagy.
CNS Neurosci Ther
January 2025
Department of Neurosurgery, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, China.
Background: Resistance to temozolomide (TMZ) remains is an important cause of treatment failure in patients with glioblastoma multiforme (GBM). ADAR1, as a member of the ADAR family, plays an important role in cancer progression and chemotherapy resistance. However, the mechanism by which ADAR1 regulates GBM progression and TMZ resistance is still unclear.
View Article and Find Full Text PDFMorusin Reverses Epithelial-Mesenchymal Transition in Gallbladder Cancer Cells by Regulating STAT3/HIF-1α Signaling.
Chem Biol Drug Des
January 2025
Department of Hepato-Biliary-Pancreatic Surgery, Shaoxing People's Hospital, Shaoxing, People's Republic of China.
Gallbladder cancer is the most prevalent malignancy of the biliary tract and has a dismal overall survival even in the present day. The development of new drugs holds promise for improving the prognosis of this lethal disease. The possible anti-neoplastic role of morusin was investigated both in vitro and in vivo.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!