The nitrile (–C 00000000000000000 00000000000000000 00000000000000000 01111111111111110 00000000000000000 01111111111111110 00000000000000000 01111111111111110 00000000000000000 00000000000000000 00000000000000000 N) functional group is a versatile pharmacophore motif that also serves as an intrinsic,…
Erschienen: The Royal Society of Chemistry, 2026-01-09
The hydrochalcone derivative MF-15 and the synthetically derived BRP-201 are potent anti-inflammatory active pharmaceutical ingredients (APIs) that suffer from poor bioavailability. This necessitates their incorporation into drug delivery systems. To address this limitation, we investigated four polymeric…
London: The Royal Society of Chemistry, 2025-10-16
Microsomal prostaglandin E 2 synthase 1 (mPGES-1) is a promising target for treating chronic inflammatory diseases and pain. The novel benzimidazole derivative AGU661 exhibits strong potency as a mPGES-1 inhibitor in a cell-free assay of prostaglandin E 2 (PGE 2 ) formation with IC 50 = 0.22 nM. Comprehensive…
Increasing life expectancy and an aging population contribute to a higher prevalence of inflammatory diseases requiring long-term treatment. Conventional anti-inflammatory drugs such as NSAIDs or COX-2 inhibitors reduce pro-inflammatory lipid mediators but also suppress essential physiological ones,…
A library of degradable poly(2-alkyl-2-oxazoline) analogues (dPOx) with different length of the alkyl substituents was characterized in detail by gradient elution liquid chromatography. The hydrophobicity increased with increased side chain length as confirmed by a hydrophobicity row, established by…
London: The Royal Society of Chemistry, 2024-10-17
Hybrid nanoparticles (HNPs) were designed by combining a PLGA core with a lipid shell that incorporated PEG–Lipid conjugates with various functionalities (-RGD, -cRGD, -NH 2 , and -COOH) to create targeted drug delivery systems. Loaded with a neutral lipid orange dye, the HNPs were extensively characterized…
In the last decades, inflammation has been recognized as being closely connected to cancer, and joint strategies encompassing chemotherapeutic and anti-inflammatory agents have been extensively studied. In this work, a series of novel cisplatin and oxaliplatin-based Pt(IV) complexes comprising non-steroidal…
Lipoxygenases (LOX) transform arachidonic acid (AA, C20:4) and docosahexaenoic acid (DHA, C22:6) into bioactive lipid mediators (LMs) that comprise not only pro-inflammatory leukotrienes (LTs) but also the specialized pro-resolving mediators (SPMs) that promote inflammation resolution and tissue regeneration.…