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| http://dx.doi.org/10.1002/anie.200905933 | DOI Listing |
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Impact of the hydrophilic-lipophilic balance of free-base and Zn(II) tricationic pyridiniumporphyrins and irradiation wavelength in PDT against the melanoma cell lines.
Eur J Med Chem
January 2025
Faculty of Biotechnology and Drug Development, University of Rijeka, Radmile Matejčić 2, Rijeka, Croatia. Electronic address:
The amphiphilic and asymmetric structure of porphyrins, when used as photosensitizers (PSs) for photodynamic therapy (PDT), has been shown through numerous previous studies to be a very important property that facilitates their entry into cells, which improves their efficiency in PDT. In this work, two groups of cationic AB pyridiniumporphyrins, free-base and chelated with Zn(II), both substituted with alkyl chains of various lengths, were studied in PDT on melanoma cell lines. The aim was to investigate the impact of hydrophilic-lipophilic balance and Zn(II) chelation, and the importance of matching the irradiation wavelength to the optical properties of the PS on in vitro PDT efficiency.
View Article and Find Full Text PDFSynthesis of cationic -acylated thiazolidine for selective activity against Gram-positive bacteria and evaluation of -acylation's role in membrane-disrupting activity.
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Department of Chemistry, School of Chemical & Biotechnology, Shanmugha Arts, Science, Technology & Research Academy (SASTRA) Deemed University Thanjavur - 613401 Tamil Nadu India
Article Synopsis
- The rise of antimicrobial-resistant strains is a major threat to existing treatments, highlighting the need for new therapies.
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Synthesis, Characterization, Bioavailability and Antimicrobial Studies of Cefuroxime-Based Organic Salts and Ionic Liquids.
Pharmaceutics
October 2024
LAQV-REQUIMTE, Department of Chemistry, NOVA School of Science and Technology, NOVA University of Lisbon, 2819-516 Caparica, Portugal.
Low oral bioavailability is a common feature in most drugs, including antibiotics, due to low solubility in physiological media and inadequate cell permeability, which may limit their efficacy or restrict their administration in a clinical setting. Cefuroxime is usually administered in its prodrug form, cefuroxime axetil. However, its preparation requires further reaction steps and additional metabolic pathways to be converted into its active form.
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Faculty of Chemical Technology, Poznan University of Technology, Berdychowo 4, Poznan 60-965, Poland.
This study is focused on the utilization of naturally occurring salicylic acid and nicotinamide (vitamin B) in the development of novel sustainable Active Pharmaceutical Ingredients (APIs) with significant potential for treating acne vulgaris. The study highlights how the chemical structure of the cation significantly influences surface activity, lipophilicity, and solubility in aqueous media. Furthermore, the new ionic forms of APIs, the synthesis of which was assessed with metrics, exhibited very good antibacterial properties against common pathogens that contribute to the development of acne, resulting in remarkable enhancement of biological activity ranging from 200 to as much as 2000 times when compared to salicylic acid alone.
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Biomolecules
June 2024
Division of Toxicology, Institute for Medical Research and Occupational Health, Ksaverska cesta 2, HR-10000 Zagreb, Croatia.
New furan, thiophene, and triazole oximes were synthesized through several-step reaction paths to investigate their potential for the development of central nervous systems (CNS)-active and cholinesterase-targeted therapeutics in organophosphorus compound (OP) poisonings. Treating patients with acute OP poisoning is still a challenge despite the development of a large number of oxime compounds that should have the capacity to reactivate acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The activity of these two enzymes, crucial for neurotransmission, is blocked by OP, which has the consequence of disturbing normal cholinergic nerve signal transduction in the peripheral and CNS, leading to a cholinergic crisis.
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