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Design, synthesis, anti-inflammatory evaluation, and molecular docking studies of novel quinazoline-4(3)-one-2-carbothioamide derivatives.
RSC Adv
January 2025
Institute of Chemistry, Vietnam Academy of Science and Technology Hanoi Vietnam
In this paper, a series of novel quinazoline-4(3)-one-2-carbothioamide derivatives (8a-p) were designed and synthesized the Wilgerodt-Kindler reaction between 2-methylquinazoline-4-one 10 and amines using S/DMSO as the oxidizing system. Their characteristics were confirmed by IR, NMR, HRMS spectra, and their melting point. These novel derivatives (8a-p) were evaluated for their anti-inflammatory activity by inhibiting NO production in lipopolysaccharide (LPS)-activated RAW 264.
View Article and Find Full Text PDFTriethylamine-mediated protonation-deprotonation unlocks dual-drug self assembly to suppress breast cancer progression and metastasis.
Proc Natl Acad Sci U S A
February 2025
Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, People's Republic of China.
Carrier-free nanomedicines exhibited significant potential in elevating drug efficacy and safety for tumor management, yet their self assembly typically relied on chemical modifications of drugs or the incorporation of surfactants, thereby compromising the drug's inherent pharmacological activity. To address this challenge, we proposed a triethylamine (TEA)-mediated protonation-deprotonation strategy that enabled the adjustable-proportion self assembly of dual drugs without chemical modification, achieving nearly 100% drug loading capacity. Molecular dynamic simulations, supported by experiment evidence, elucidated the underlying self-assembly mechanism.
View Article and Find Full Text PDFNovel Nonaqueous PD/PZ/NMP Absorbent for Energy-Efficient CO Capture: Insights into the Crystal-Phase Regulation Mechanism of the Powdery Product.
Environ Sci Technol
January 2025
School of Environmental Science and Engineering, Shenzhen Key Laboratory of Municipal Solid Waste Recycling Technology and Management, Southern University of Science and Technology, Shenzhen 518055, China.
Solid-liquid biphasic absorbents are a promising solution for overcoming the high-energy consumption challenge faced by liquid amine-based CO capture technologies. However, their practical applications are often hindered by difficulties in separating viscous solid-phase products. This study introduces a novel nonaqueous absorbent system (PD/PZ/NMP) composed of 4-amino-1-methylpiperidine (PD), piperazine (PZ), and -methyl-2-pyrrolidone (NMP), engineered to produce easily separable powdery products.
View Article and Find Full Text PDFThe selective amination of aromatic C-H bonds is a powerful strategy to access aryl amines, functionalities found in many pharmaceuticals and agrochemicals. Despite advances in the field, a platform for the direct, selective C-H amination of electronically diverse (hetero)arenes, particularly electron-deficient (hetero)arenes, remains an unaddressed fundamental challenge. In addition, many (hetero)arenes present difficulty in common selective pre-functionalization reactions, such as halogenation, or metal-catalyzed borylation and silylation.
View Article and Find Full Text PDFInterrupted borrowing hydrogen strategy enabled aminomethylation and direct cross-dehydrogenative coupling strategy enabled dicarbonylation reactions of imidazo[1,5-]pyridines.
Chem Commun (Camb)
January 2025
Natural Products and Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu & Kashmir, 180001, India.
Herein, we disclose the development of novel aminomethylation and dicarbonylation reactions of imidazo[1,5-]pyridines. The developed aminomethylation strategy involves a Pd-catalyzed interrupted borrowing hydrogen strategy by utilizing MeOH as the methylene source. A wide variety of imidazo[1,5-]pyridines and secondary amines were explored for the developed strategy.
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