Fluorescent bioimaging is a crucial technique for studies in real cell samples, providing vital information about the metabolism of ions or molecules of biological and pharmaceutical significance. This technique typically uses probes based on organic small-molecule fluorophores, with N-heteroaromatic scaffolds playing an essential role due to their exceptional electronic properties and biocompatibility. Among these, pyrazole derivatives stand out as particularly promising due to their high synthetic versatility and structural diversity. This review highlights prominent examples from the period 2020-2024, focusing on the chemistry, properties, and bioimaging applications of fluorescent pyrazole derivatives. By highlighting the latest advancements in this field, this manuscript aims to inspire and motivate researchers, emphasizing the potential impact of this work on the future of bioimaging.
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http://dx.doi.org/10.1039/d4ra07485h | DOI Listing |
Sci Rep
December 2024
Laboratory of Bioinorganic Chemistry, Department of Pharmacy and Biotechnology, University of Bologna, 40127, Bologna, Italy.
This manuscript details the application of Isothermal Titration Calorimetry (ITC) to characterize the kinetics of 3CL, the main protease from the Severe Acute Respiratory Syndrome CoronaVirus-2 (SARS-CoV-2), and its inhibition by Ensitrelvir, a known non-covalent inhibitor. 3CL is essential for producing the proteins necessary for viral infection, which led to the COVID-19 pandemic. The ITC-based assay provided rapid and reliable measurements of 3CL activity, allowing for the direct derivation of the kinetic enzymatic constants K and k by monitoring the thermal power required to maintain a constant temperature as the substrate is consumed.
View Article and Find Full Text PDFEur J Med Chem
December 2024
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, 144411, India. Electronic address:
This study presents a comprehensive exploration of the synthesis of novel compounds targeting Chagas Disease (CD) caused by Trypanosoma cruzi. It is a global health threat with over 6-7 million infections worldwide. Addressing challenges in current treatments, the investigation explores diverse compound classes, including thiazoles, thiazolidinone, imidazole, pyrazole, 1,6-diphenyl-1H-pyrazolo[3,4-b] pyridine, pyrrole, naphthoquinone, neolignan, benzeneacyl hydrazones, and chalcones-based compounds.
View Article and Find Full Text PDFChem Biol Drug Des
January 2025
Jiangxi Provincial Key Laboratory of Synthetic Pharmaceutical Chemistry, Gannan Normal University, Ganzhou, China.
RET (Rearranged during transfection) kinase is a validated target for non-small cell lung cancer (NSCLC). In 2020, two selective RET inhibitors, selpercatinib and pralsetinib were approved by the US FDA. However, high treatment costs and clinically acquired resistance (e.
View Article and Find Full Text PDFNat Commun
December 2024
Department of Infectious Diseases, School of Immunology & Microbial Sciences, King's College London, London, SE1 9RT, UK.
The role of myeloid cells in the pathogenesis of SARS-CoV-2 is well established, in particular as drivers of cytokine production and systemic inflammation characteristic of severe COVID-19. However, the potential for myeloid cells to act as bona fide targets of productive SARS-CoV-2 infection, and the specifics of entry, remain unclear. Using a panel of anti-SARS-CoV-2 monoclonal antibodies (mAbs) we performed a detailed assessment of antibody-mediated infection of monocytes/macrophages.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
Applied Organic Chemistry Department, National Research Center, Dokki, Cairo 12622, Egypt; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Pharos University in Alexandria, Canal El Mahmoudia St., Alexandria 21648, Egypt. Electronic address:
The current research focuses on the design and synthesis of celecoxib analogues incorporating sulphonamide pyrazole moieties 4, 5, 6a-e, and 7a-f with the aim of achieving a broad range of COX-2 selectivity in vitro. Among these, compounds 6b-d, 7a, 7e, and 7d exhibited potent inhibition, with IC values ranging between 0.05 and 0.
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