Prodrugs are increasingly used as delivery vehicles for pharmaceutical agents that present solubility and/or pharmacokinetic/metabolic issues. In the course of the development of prodrugs for the antitumoral agent thiocoraline, standard coupling reagents and procedures failed to provide the desired target derivatives because of the lack of reactivity of its quinolinic alcohol. In contrast, the use of N,N,N',N'-tetramethylchloroformamidinium hexafluorophosphate (TCFH) resulted in good yields of ester prodrugs of thiocoraline and could be applicable to other drugs with similar limitations.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/bc8002327 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
The effect of photoinitiator systems on resin-based composite containing ZnO-nanoparticles.
Dent Mater
December 2024
Division of Dentistry, School of Medical Sciences, University of Manchester, Manchester, UK; Photon Science Institute, University of Manchester, Manchester, UK. Electronic address:
Objective: Zinc oxide (ZnO) powder possesses antibacterial activity and although white in color, it can severely reduce the depth of cure (DoC) of resin-based composite (RBC). This study investigated the effect of unary and binary photoinitiator systems on the DoC and degree of conversion (DC) of formulated RBC containing ZnO-nanoparticles.
Methods: Fourteen RBCs (n = 3/group) were formulated consisting of 50 wt% mixture of monomers (Bis-GMA, TEGDMA, and UDMA) and 50 wt% fillers (inert barium glass powder and silica nanoparticles).
Inorganic-Dominated Interphase Enabled by Tuning Solvation Configuration for 4.8 V Lithium-Ion Batteries.
J Phys Chem Lett
December 2024
School of Advanced Materials, Peking University Shenzhen Graduate School, Shenzhen 518055, China.
Constructing a dense inorganic component-dominated cathode electrolyte interphase (CEI) to meet the long-term cycling requirements of ultrahigh voltage cathodes has been a crucial challenge. Nevertheless, this goal is difficult to achieve in traditional electrolyte compositions due to the inevitable decomposition of organic solvents. Herein, by utilizing the localized mismatch between the strongly coordinating hexafluorophosphate anion (PF) and the weakly coordinating solvent 1,1,1-trifluoro-,-dimethylmethanesulfonamide (TFDMSA), abundant aggregates (AGGs) emerged under a regular Li salt concentration of 1 m lithium bis(fluorosulfonyl)imide (LiFSI) + 0.
View Article and Find Full Text PDFImproving the Cycling Stability of NCM811 at High-Voltage 4.5V in Ester-Based Electrolytes with LiDFOB.
Small Methods
December 2024
State Key Laboratory for Mechanical Behavior of Materials, Xi'an Jiaotong University, 28 Xianning West Road, Xi'an, 710049, China.
Nickel-rich layered cathode materials, particularly LiNiMnCoO (NCM811), have garnered significant attention due to their high energy density and impressive electrochemical performance. However, their cycling stability is compromised at elevated voltages, primarily due to structural instability and interfacial degradation. In this study, lithium difluoro(oxalato)borate (LiDFOB) is introduced into a commercial electrolyte based on lithium hexafluorophosphate (LiPF) to elucidate the structural and interfacial changes occurring in NCM811 at a high cut-off voltage of 4.
View Article and Find Full Text PDFPhenothiazine Derivative-Based Photoinitiators for Ultrafast Sunlight-Induced Free Radical Polymerization and Rapid Precision 3D Printing.
ACS Appl Mater Interfaces
December 2024
Université de Haute-Alsace, CNRS, IS2M UMR7361, F-68100 Mulhouse, France.
Article Synopsis
- The study presents twenty-six new phenothiazine derivatives designed to serve as photoinitiators for free radical polymerization, enabling effective reactions under visible light and sunlight when combined with an amine and an iodonium salt.
- The new photoinitiating systems demonstrated impressive double bond conversions of up to 87% under specific light conditions, significantly outperforming a commercial reference system, particularly under sunlight.
- The findings highlight the potential for these systems in environmentally friendly 3D printing and other curing applications, promoting efficient polymerization in both artificial and natural light settings.
Development of a Triazinyluronium-Based Dehydrative Condensing Reagent with No Heteroatomic Bonds.
J Org Chem
December 2024
Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical, and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.
Article Synopsis
- A new dehydrative condensing reagent, DMT-TU, has been created, which is based on triazinyluronium.
- DMT-TU is safer than traditional reagents since it lacks high-energy N-N and N-O bonds, making it less explosive according to differential scanning calorimetry.
- The reagent successfully converts carboxylic acids and amines into amides at room temperature and minimizes racemization in peptide bond formation.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!