Aminothiazole-based inhibitors designed for HCV polymerase display low micromolar potencies in biochemical assays. These compounds show a stringent preference for a cyclohexyl hydrophobe at the 2-amino position. The composition of these compounds suggests that they may be interacting at a recently discovered allosteric site on the polymerase.
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http://dx.doi.org/10.1016/j.bmcl.2004.10.024 | DOI Listing |
Bioorg Med Chem Lett
February 2025
The Third Affiliated Hospital of Zhejiang Chinese Medical University, Hangzhou, Zhejiang 310000, China. Electronic address:
Arch Biochem Biophys
December 2024
Institute of Biotechnology, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
Nootkatone, a sesquiterpenoid widely used in the food and cosmetics industries, exhibits diverse biological activities and pharmaceutical prospects. Modification of nootkatone to create new derivatives with desirable activities has attracted significant attention. For this purpose, cytochrome P450 monooxygenases (P450 or CYP) are attractive candidates due to their ability to perform regio- and stereoselective hydroxylation at allylic C-H bonds.
View Article and Find Full Text PDFArch Biochem Biophys
November 2024
Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, 26470, Türkiye.
In this study, thiazole derivatives containing sulphonamide, amide, and phenyl amino groups were synthesized to protect the free amino groups of 5-methyl-4-phenyl-2-aminothiazole and 4-phenyl-2-aminothiazole. Halogenated reactions of N-protected thiazole derivatives have been investigated. LCMS, FT-IR, H NMR, and C NMR spectroscopy techniques were used to elucidate the structures of the synthesized compounds.
View Article and Find Full Text PDFJ Med Chem
August 2024
Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
COP9 signalosome catalytic subunit CSN5 plays a key role in tumorigenesis and tumor immunity, showing potential as an anticancer target. Currently, only a few CSN5 inhibitors have been reported, at least partially, due to the challenges in establishing assays for CSN5 deubiquitinase activity. Here, we present the establishment and validation of a simple and reliable non-catalytic activity assay platform for identifying CSN5 inhibitors utilizing a new fluorescent probe, , that exhibits enhanced fluorescence and fluorescence polarization features upon binding to CSN5.
View Article and Find Full Text PDFJ Phys Chem B
June 2024
BASF Coatings GmbH, Glasuritstrasse 1, Münster 48165, Germany.
A computational study was performed to investigate the dynamics of aqueous electrolytes containing organic corrosion inhibitors near electrified interfaces by using the constant-charge model in classical molecular dynamics simulations. The results showed that when inhibitors form films at the interface, the surface charge of the electrode causes displacement of the molecules, referred to as electroporation. The hydrophobicity of the inhibitor molecules affects both the stability of the films and their recovery time.
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