An efficient functionalization of ortho-C(sp(2))-H bonds of picolinamide (PA)-protected benzylamine substrates with a range of vinyl iodides as well as acetylenic bromide is reported. ortho-Phenyl benzoic acid (oPBA) acts as an effective promoter in this reaction system. This method provides a practical strategy to access highly functionalized benzylamine compounds for organic synthesis.
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http://dx.doi.org/10.1021/ol301214u | DOI Listing |
Viruses
December 2024
Department of Medical Laboratory Science and Biotechnology, Asia University, Taichung 41354, Taiwan.
This study investigated a library of known and novel glycyrrhizic acid (GL) conjugates with amino acids and dipeptide esters, as inhibitors of the DENV NS2B-NS3 protease. We utilized docking algorithms to evaluate the interactions of these GL derivatives with key residues (His51, Asp75, Ser135, and Gly153) within 10 Å of the DENV-2 NS2B-NS3 protease binding pocket (PDB ID: 2FOM). It was found that compounds and exhibited unique binding patterns, forming hydrogen bonds with Asp75, Tyr150, and Gly153.
View Article and Find Full Text PDFSensors (Basel)
December 2024
School of Instrument and Electronics, North University of China, Taiyuan 030051, China.
Tire pressure monitoring systems (TPMSs) are essential for maintaining driving safety by continuously monitoring critical tire parameters, such as pressure and temperature, in real time during vehicle operation. Among these parameters, tire pressure is the most significant, necessitating the use of highly precise, cost-effective, and energy-efficient sensing technologies. With the rapid advancements in micro-electro-mechanical system (MEMS) technology, modern automotive sensing and monitoring systems increasingly rely on MEMS sensors due to their compact size, low cost, and low power consumption.
View Article and Find Full Text PDFSensors (Basel)
December 2024
Division de Fotónica, Centro de Investigaciones en Óptica AC, Loma del Bosque 115, Col. Lomas del Campestre, León 37150, Guanajuato, Mexico.
Methylene blue is a cationic organic dye commonly found in wastewater, groundwater, and surface water due to industrial discharge into the environment. This emerging pollutant is notably persistent and can pose risks to both human health and the environment. In this study, we developed a Surface Plasmon Resonance Biosensor employing a BK7 prism coated with 3 nm chromium and 50 nm of gold in the Kretschmann configuration, specifically for the detection of methylene blue.
View Article and Find Full Text PDFPharmaceutics
December 2024
Dipartimento di Farmacia, Salute e Scienze della Nutrizione, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, Italy.
Hypertension affects 32% of adults worldwide, leading to a significant global consumption of cardiovascular medications. Atenolol, a β-adrenergic receptor blocker, is widely prescribed for cardiovascular diseases such as hypertension, angina pectoris, and myocardial infarction. According to the Biopharmaceutics Classification System (BCS), atenolol belongs to Class III, characterized by high solubility but low permeability.
View Article and Find Full Text PDFPharmaceutics
November 2024
Department of Analytical Chemistry, Faculty of Pharmacy, Medical University of Lodz, 90-419 Lodz, Poland.
Background: The penetration of drugs through the blood-brain barrier is one of the key pharmacokinetic aspects of centrally acting active substances and other drugs in terms of the occurrence of side effects on the central nervous system. In our research, several regression models were constructed in order to observe the connections between the active pharmaceutical ingredients' properties and their bioavailability in the CNS, presented in the form of the log BB parameter, which refers to the drug concentration on both sides of the blood-brain barrier.
Methods: Predictive models were created using the physicochemical properties of drugs, and multiple linear regression and a data mining method, i.
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