A C-terminal amidothiourea motif is shown to promote a β-turn-like folded conformation in a series of β-amino acid-based short peptides in both the solid state and solution phase by an intramolecular 11-membered ring hydrogen bond.
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http://dx.doi.org/10.1021/acs.joc.0c01139 | DOI Listing |
ChemSusChem
January 2025
Polish Academy of Sciences, Institute of Organic Chemistry, Kasprzaka 44/52, 01-224, Warsaw, POLAND.
We demonstrate the application of mechanochemistry in the synthesis of indolone-based photoswitches (hemiindigos, hemithioindigos, and oxindoles) via Knoevenagel condensation reactions. Utilizing ball-milling and an organic base (piperidine) acting as catalyst and solvent for liquid assisted grinding (LAG) conditions, we achieve rapid, solvent-free transformations, obtaining a set of known and previously unreported photoswitches, including highly functional amino acid-based photoswitches, multichromophoric derivatives and photoswitchable cavitands based on resorcin[4]arenes. The reaction under mechanochemical conditions gives moderate-to-high yields and is highly stereoselective leading to Z-isomers of hemiindigos and hemithioindigos and E-isomers of oxindoles.
View Article and Find Full Text PDFInt J Nanomedicine
January 2025
School of Medicine, Huaqiao University, Quanzhou, Fujian, People's Republic of China.
The effective clinical translation of messenger RNA (mRNA), small interfering RNA (siRNA), and microRNA (miRNA) for therapeutic purposes hinges on the development of efficient delivery systems. Key challenges include their susceptibility to degradation, limited cellular uptake, and inefficient intracellular release. Polymeric drug conjugates (PDCs) offer a promising solution, combining the benefits of polymeric carriers and therapeutic agents for targeted delivery and treatment.
View Article and Find Full Text PDFInt J Nanomedicine
January 2025
Department of Medicine, Surgery and Pharmacy, University of Sassari, Sassari, Italy.
Purpose: Dimethyl fumarate (DMF), the first-line oral therapy for relapsing-remitting multiple sclerosis, is rapidly metabolized into monomethyl fumarate. The DMF oral administration provokes gastrointestinal discomfort causing treatment withdrawal. The present study aimed to develop an innovative formulation for DMF nasal administration.
View Article and Find Full Text PDFGlob Chall
January 2025
Department of Radiation Oncology Cancer Center of Peking University Third Hospital Peking University Third Hospital Haidian, 49 Huayuan North Road Beijing 100191 China.
Hepatocellular carcinoma (HCC) stands as the predominant form of primary liver cancer, characterized by a dismal prognosis. Therapeutic options for advanced HCC remain sparse, with efficacy significantly hampered by the emergence of drug resistance. In parallel with research into novel pharmacological agents, advances in drug delivery systems represent a promising avenue for overcoming resistance.
View Article and Find Full Text PDFInorg Chem
January 2025
Research Institute for Electronic Science, Hokkaido University, Sapporo 001-0021, Japan.
Electrochemical devices that can operate at temperatures of 200-300 °C are expected to become the next-generation energy conversion devices in fuel cells and electrosynthesis, which are important for achieving carbon neutrality. Proton conductors based on phosphate glasses are being developed as candidate materials for such devices. We recently developed a glass proton conductor by using silicophosphoric acid based on the idea of solidifying phosphoric acid with silicon as a cross-linking glass framework.
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