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Synthesis, biological evaluation, and in silico studies of phenyl naphthalene-2-sulfonate derived thiosemicarbazones as potential carbonic anhydrase inhibitors.
Bioorg Chem
January 2025
Institute of Chemical Sciences, Bahauddin Zakariya University, 60800 Multan, Pakistan. Electronic address:
A series of novel phenyl naphthalene-2-sulfonate-based thiosemicarbazones (5a-v) were synthesized and evaluated for their inhibitory activity against human carbonic anhydrases I and II (hCA I and hCA II). Compounds 5d and 5p demonstrated the highest inhibitory potency, with IC values of 4.32 ± 0.
View Article and Find Full Text PDF[A commentary: New carbonic anhydrase IX-targeted probes for imaging hypoxic tumors].
Bull Cancer
December 2024
Département de biologie expérimentale des tumeurs, institut de carcinogenèse, centre national de recherche médicale en oncologie N.N. Blokhin, ministère de la Santé de Russie, 24 Kashirskoe shosse, Moscou 115522, Fédération de Russie. Electronic address:
In 2023, the journals "Bioconjugate Chemistry" and "Sensors and Actuators B: Chemical" published two papers describing new biosensors for imaging hypoxic regions in tumors. Cao et al. combined acetazolamide (AZA) to target carbonic anhydrase IX (CA IX) with two tyrosine-derived Mn(II)-ethylenediaminetetraacetic acid chelates (TyEDTA) on a rigid triazine (TA) scaffold.
View Article and Find Full Text PDFNovel Dibenzoazepine-Substituted Triazole Hybrids as Cholinesterase and Carbonic Anhydrase Inhibitors and Anticancer Agents: Synthesis, Characterization, Biological Evaluation, and Studies.
ACS Omega
November 2024
Department of Medical Biology, Faculty of Medicine, Çanakkale Onsekiz Mart University, 17020 Çanakkale, Türkiye.
The new dibenzoazepine-substituted triazole hybrids (-) were designed by molecular hybridization approach and synthesized utilizing the Cu(I)-catalyzed click reaction. The hybrid structures (-) were obtained in high yields (74-98%) with a simple two-step synthesis strategy and fully characterized. These compounds were assessed for their influence on various metabolic enzymes including human carbonic anhydrase isoenzymes (hCA I and hCA II), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE).
View Article and Find Full Text PDFNovel Hydrazide-Hydrazones Bearing a Benzimidazole Ring: Design, Synthesis, and Evaluation of Inhibitor Properties Against CA I and CA II Isozymes.
Chem Biol Drug Des
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.
In this study, we propose identifying potential novel compounds targeting carbonic anhydrase I and II. Herein, we have designed and synthesized new benzimidazole-hydrazide-hydrazones derivatives (4a-4r) to investigate the effects of these synthesized compounds on CA isoenzymes. The compounds' H NMR, C NMR, and HRMS spectra were used to confirm their chemical structures.
View Article and Find Full Text PDFRelaxation-exchange magnetic resonance imaging (REXI): a non-invasive imaging method for evaluating trans-barrier water exchange in the choroid plexus.
Fluids Barriers CNS
November 2024
Interdisciplinary Institute of Neuroscience and Technology and Liangzhu Laboratory, Zhejiang University School of Medicine, Hangzhou, China.
Background: The choroid plexus (CP) plays a crucial role in cerebrospinal fluid (CSF) production and brain homeostasis. However, non-invasive imaging techniques to assess its function remain limited. This study was conducted to develop a novel, contrast-agent-free MRI technique, termed relaxation-exchange magnetic resonance imaging (REXI), for evaluating CP-CSF water transport, a potential biomarker of CP function.
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