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You Win Some, You Lose Some: Modifying the Molecular Periphery of Nitrofuran-Tagged Diazaspirooctane Reshapes Its Antibacterial Activity Profile.
Int J Mol Sci
December 2024
Department of Medical Chemistry, Institute of Chemistry, Saint Petersburg State University, Saint Petersburg 199034, Russia.
The use of the concept of privileged structures significantly accelerates the search for new leads and their optimization. 6-(methylsulfonyl)-8-(4-methyl-4-1,2,4-triazol-3-yl)-2-(5-nitro-2-furoyl)-2,6-diazaspiro[3.4]octane has been identified as a lead, with MICs of 0.
View Article and Find Full Text PDFMulticationic ruthenium phthalocyanines as photosensitizers for photodynamic inactivation of multiresistant microbes.
Eur J Med Chem
December 2024
Departamento de Química Orgánica, Universidad Autónoma de Madrid, Cantoblanco, 28049, Madrid, Spain; Institute for Advanced Research in Chemical Sciences (IAdChem), Universidad Autónoma de Madrid, Cantoblanco, 28049, Madrid, Spain. Electronic address:
Four photosensitizers PS1a-PS4a consisting in multicationic ruthenium(II) phthalocyanines (RuPcs) have been evaluated in photodynamic inactivation (PDI) of multiresistant microorganisms. The RuPcs, bearing from 4 to 12 terminal ammonium salts, have been designed to target the microorganisms cytoplasmic cell membrane and display high singlet oxygen quantum yields. In addition, PS3a and PS4a were conceived to exhibit multi-target localization by endowing them with amphiphilic character, using two different structural approaches.
View Article and Find Full Text PDFA generalisable risk factor: Socioeconomic status and multi-resistant organism colonisation.
Clin Infect Dis
December 2024
Adelaide Medical School, The University of Adelaide, Adelaide SA 5005, Australia.
LEGO-Lipophosphonoxin membrane activity is enhanced by presence of phosphatidylethanolamine but hindered by outer membrane.
Sci Rep
January 2025
Department of Genetics and Microbiology, Faculty of Science, Charles University, Viničná 5, 128 00, Prague, Czech Republic.
Finding effective antibiotics against multi-resistant strains of bacteria has been a challenging race. Linker-Evolved-Group-Optimized-Lipophosphonoxins (LEGO-LPPOs) are small modular synthetic antibacterial compounds targeting the cytoplasmic membrane. Here we focused on understanding the reasons for the variable efficacy of selected LEGO-LPPOs (LEGO-1, LEGO-2, LEGO-3, and LEGO-4) differing in hydrophobic and linker module structure and length.
View Article and Find Full Text PDFNematode-bacteria interactions in bovine parasitic otitis.
Rev Bras Parasitol Vet
January 2025
Laboratório de Helmintologia Romero Lascasas Porto, Departamento de Microbiologia, Imunologia e Parasitologia, Universidade do Estado do Rio de Janeiro - UERJ, Rio de Janeiro, RJ, Brasil.
Bovine parasitic otitis poses challenges in diagnosis, treatment and involves various agents, such as bacteria, fungi, mites, and nematodes. This study focused on the nematodes and bacteria isolated from the auditory canals of dairy cattle. A total of twenty samples were collected from dairy cattle in two states of Brazil.
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