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Antimicrobial peptides (AMPs) are small, positively charged biomolecules produced by various organisms such as animals, microbes, and plants. These AMPs play a significant role in defense mechanisms and protect from adverse conditions. The emerging problem of drug resistance in microbes poses a global health challenge in treating diseases.

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Compounds containing the piperidine group are highly attractive as building blocks for designing new drugs. Functionalized piperidines are of significant interest due to their prevalence in the pharmaceutical field. Herein, 3-oxo-3-(piperidin-1-yl) propanenitrile has been synthesized, and piperidine-based sodium alginate/poly(vinyl alcohol) films have been prepared.

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Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties.

Eur J Med Chem

December 2024

School of Pharmacy and Food Engineering, Wuyi University, 529020, Jiangmen, China; Department of Chemistry, University of Liverpool, L69 7ZD, Liverpool, UK. Electronic address:

Aryl quinolone derivatives can target the cytochrome bc complex of Plasmodium falciparum, exhibiting excellent in vitro and in vivo antimalarial activity. However, their clinical development has been hindered due to their poor aqueous solubility profiles. In this study, a series of bioisosteres containing saturated heterocycles fused to a 4-pyridone ring were designed to replace the inherently poorly soluble quinolone core in antimalarial quinolones with the aim to reduce π-π stacking interactions in the crystal packing solid state, and a synthetic route was developed to prepare these alternative core derivatives.

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Novel inhibition of sortase A by plantamajoside: implications for controlling multidrug-resistant infections.

Appl Environ Microbiol

December 2024

Department of Gastrocolorectal Surgery, General Surgery Center, The First Hospital of Jilin University, Changchun, Jilin, China.

Article Synopsis
  • The research introduces plantamajoside (PMS) as an innovative inhibitor of sortase A (SrtA), an enzyme crucial for the virulence of methicillin-resistant Staphylococcus aureus (MRSA), showcasing its potential in combating multi-drug resistant pathogens.
  • PMS effectively reduces MRSA's ability to adhere to surfaces and form biofilms, leading to increased survival rates in infected cell models and proving beneficial in animal models by lowering mortality rates and bacterial loads.
  • The findings emphasize the significance of targeting specific bacterial mechanisms, such as SrtA, to develop new therapeutic strategies against antibiotic-resistant infections, particularly MRSA.
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Article Synopsis
  • Acinetobacter baumannii, especially the carbapenem-resistant strains (CRAB), is a critical pathogen linked to antimicrobial resistance (AMR) and is prioritized by the WHO.
  • Phage therapy is being explored as a potential treatment for CRAB infections due to increasing resistance to conventional antibiotics.
  • A newly isolated lytic phage, vAbaIN10, exhibits effective lytic activity against CRAB in various conditions and shows promise in advancing treatment options for multidrug-resistant infections.
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