A series of 2-ethoxycarbonylthieno[2,3-]quinolines were synthesized in the bio-derived "green" solvent γ-valerolactone (GVL) and evaluated for their inhibitory activities against PTP1B, the representative compound 6a displayed an IC value of 8.04 ± 0.71 μM with 4.34-fold preference over TCPTP. These results provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8694002 | PMC |
http://dx.doi.org/10.1039/d0ra09247a | DOI Listing |
Int J Biol Macromol
January 2025
College of Food Science and Nutritional Engineering, China Agricultural University, Beijing 100083, China; National Engineering Research Center for Fruit and Vegetable Processing, Key Lab of Fruit and Vegetable Processing, Ministry of Agriculture, Beijing, China.
This study utilized deep eutectic solvents (DES) based on choline chloride/lactic acid (ChCl/LA) to deconstruct coconut fibers. The effects of DES with different temperatures and molar ratios on the yield of lignin, recovery rate of residues, structural changes in lignin and solid residues, and saccharification efficiency were investigated. The results showed that acidic DES treatment effectively deconstructed the coconut fibers, resulting in a high lignin yield of 68.
View Article and Find Full Text PDFTalanta
January 2025
Pharmaceutical Chemistry Research Laboratory I, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, 221005, India. Electronic address:
The cholinergic deficits and amyloid beta (Aβ) aggregation are the mainstream simultaneously observed pathologies during the progression of Alzheimer's disease (AD). Deposited Aβ plaques are considered to be the primary pathological hallmarks of AD and are contemplated as promising diagnostic biomarker. Herein, a series of novel theranostic agents were designed, synthesised and evaluated against cholinesterase (ChEs) enzymes and detection of Aβ species, which are major targets for development of therapeutics for AD.
View Article and Find Full Text PDFJ Colloid Interface Sci
January 2025
State Key Laboratory of Biobased Fiber Manufacturing Technology, China Light Industry Key Laboratory of Papermaking and Biorefinery, Tianjin Key Laboratory of Pulp and Paper, Tianjin University of Science and Technology, Tianjin 300457, China. Electronic address:
Exploring innovative and sustainable routes for the production of biodegradable biomass-based materials is critical to promote a circular carbon economy and carbon neutrality goals. Fossil-based non-biodegradable plastic waste poses a nonnegligible threat to humans and the ecological environment, and biomass-based functional materials are becoming increasingly viable alternatives. Lignin, a naturally occurring macromolecular polymer, is green and renewable resource rich in aromatic rings, with biodegradability, biocompatibility, and excellent processability for eco-friendly composites.
View Article and Find Full Text PDFJ Pharm Biomed Anal
January 2025
Sabanci University Nanotechnology Research and Application Center (SUNUM), Istanbul 34956, Turkey.
This study aimed to determine the chromatographic retention and dissociation/protonation constant (pK) values of lapatinib and tamoxifen, key drugs used in metastatic breast cancer treatment, at 37°C using both conventional and green high-performance liquid chromatography (HPLC) methods. Qualitative analysis was conducted on an XTerra C18 column (250 ×4.6 mm I.
View Article and Find Full Text PDFJ Colloid Interface Sci
January 2025
Research Center for Advanced Science and Technology, The University of Tokyo, 4-6-1 Komaba, Meguro-ku, 153-8904, Tokyo, Japan; Institute of Industrial Science, The University of Tokyo, 4-6-1 Komaba, Meguro-ku, 153-8505, Tokyo, Japan. Electronic address:
Phase separation, a fundamental phenomenon in both natural and industrial settings, involves the coarsening of domains over time t to reduce interfacial energy. While well-understood for simple viscous liquid mixtures, the physical laws governing coarsening dynamics in complex fluids, such as colloidal suspensions, remain unclear. Here, we investigate colloidal phase separation through particle-based simulations with and without hydrodynamic interactions (HIs).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!