Combining the Ugi reaction with ring opening reaction of furans for the synthesis of novel isoquinolinone and 1,2-dihydroisoquinoline scaffolds has been developed. The isoquinolinone and 1,2-dihydroisoquinoline derivatives with unsaturated carbonyl moiety may open up many opportunities for further functionalizations.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1007/s11030-013-9434-1 | DOI Listing |
Adv Med Sci
January 2025
Department of Histology and Embryology, Faculty of Medicine, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Toruń, Poland; Faculty of Medicine, Collegium Medicum, Mazovian Academy in Płock, Płock, Poland.
Purpose: Proper functioning of the endothelial barrier is crucial for cardiovascular system homeostasis. Oxidative stress can lead to endothelial dysfunction (ED), damaging lipids, proteins, and DNA. Reactive oxygen species also increase cytoplasmic Ca levels, activating transient receptor potential melastatin 2 (TRPM2), a membrane non-selective calcium channel.
View Article and Find Full Text PDFNat Commun
December 2024
Key Laboratory of Green Chemistry & Technology, Ministry of Education, College of Chemistry, Sichuan University, Chengdu, 610064, China.
The activation of C-C bond of benzocyclobutenones under mild reaction conditions remains a challenge. We herein report a photoinduced catalyst-free regio-specific C1-C8 bond cleavage of benzocyclobutenones, enabling the generation of versatile ortho-quinoid ketene methides for aza-[4 + 2]-cycloaddition with imines, which offers a facile route to isoquinolinone derivatives, including seven family members of protoberberine alkaloids, gusanlung A, B, D, 8-oxotetrahydroplamatine, tetrahydrothalifendine, tetrahydropalmatine, and xylopinine. Furthermore, the catalytic enantioselective version of this strategy is also realized by merging synergistic photocatalysis and chiral Lewis acid catalysis.
View Article and Find Full Text PDFJ Biol Chem
December 2024
Institute of Biomedicine, University of Turku, Turku, Finland. Electronic address:
Enzyme promiscuity is the ability of an enzyme to catalyze an unexpected side reaction in addition to its main reaction. Here, we describe a biocatalytic process to produce nonhydrolyzable NAD+ analogs based on the ADP-ribosyltransferase activity of pertussis toxin PtxS1 subunit. First, in identical manner to normal catalysis, PtxS1 activates NAD+ to form the reactive oxocarbenium cation.
View Article and Find Full Text PDFJ Chem Inf Model
January 2025
Medicinal Chemistry Laboratory II, Gedeon Richter Plc., Gyömrői út 19-21, Budapest 1103, Hungary.
The significant importance of GABA receptors in the treatment of central nervous system (CNS) disorders has been known for a long time. However, only in recent years have experimental protein structures been published that can open the door to understanding protein-ligand interactions and may effectively help the rational drug design for the future. In our previous work (Szabó, G.
View Article and Find Full Text PDFInt J Mol Sci
October 2024
Department of Chemical, Biological, Pharmaceutical, and Environmental Sciences, University of Messina, Viale Ferdinando Stagno d'Alcontres 31, 98166 Messina, Italy.
In the eukaryotic cells, the ubiquitin-proteasome system (UPS) plays a crucial role in the intracellular protein turnover. It is involved in several cellular functions such as the control of the regular cell cycle progression, the immune surveillance, and the homeostasis. Within the 20S proteasome barrel-like structure, the catalytic subunits, β1, β2 and β5, are responsible for different proteolytic activities: caspase-like (C-L), trypsin-like (T-L) and chymotrypsin-like (ChT-L), respectively.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!