A green, facile and tunable pair electrochemical process was developed for the synthesis of new benzenesulfonamide derivatives by using reductive controlled potential electrolysis of dinitrobenzene (DNB) in the presence of arylsulfinic acids (ASAs). In addition to the usual features associated with paired electrochemical methods, eg high energy efficient, this method has a tunable characteristic, so that, by adjusting the potential, different products can be synthesized. By applying the potential of -0.4 V vs. Ag/AgCl, N-hydroxy-N-(4-nitrophenyl)benzenesulfonamide derivatives are selectively formed, while, by applying the potential of -1.1 V vs. Ag/AgCl, the final products are N-(4-amino-3-(phenylsulfonyl)phenyl) benzenesulfonamide derivatives. This work beautifully shows the potential applications of the electrochemistry as a powerful tool for the synthesis of organic compounds.
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http://dx.doi.org/10.1038/s41598-019-38544-4 | DOI Listing |
J Med Chem
January 2025
Biomedical Research Division, Korea Institute of Science and Technology (KIST), Seoul 02792, Republic of Korea.
Carbonic anhydrases (CAs) IX and XII are crucial for the survival and metastasis of solid tumors under hypoxic conditions. We designed compounds -, integrating triazole and benzenesulfonamide scaffolds known for inhibiting tumor-associated CAs IX/XII. Initial synthesis included compounds -, followed by diversification with small hydrophobic groups (-) and hydrophilic heterocyclic secondary amines (-).
View Article and Find Full Text PDFJ Biochem Mol Toxicol
January 2025
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Guwahati, India.
This study is focused on the design, synthesis, and evaluation of some sulfonamide derivatives for their inhibitory effects on human carbonic anhydrase (hCA) enzymes I, II, IX, and XII as well as for their antioxidant activity. The purity of the synthesized molecules was confirmed by the HPLC purity analysis and was found in the range of 93%-100%. The inhibition constant (K) against hCA I ranged from 0.
View Article and Find Full Text PDFBlood Cancer J
January 2025
School of Medicine, Faculty of Medicine and Health Sciences, Tel Aviv University, Tel Aviv, Israel.
Fedratinib is a predominantly JAK2 inhibitor that has shown efficacy in untreated and ruxolitinib-exposed patients with myelofibrosis (MF). Based on randomized clinical trial data, it is approved for use in patients with International Prognostic Scoring System (IPSS) or Dynamic International Prognostic Scoring System (DIPSS) intermediate-2 or high-risk disease and is distinguished from ruxolitinib in that it can be administered without dose reduction in patients with thrombocytopenia, to a platelet count above 50,000/µL. In these trials, fedratinib achieved significant spleen volume reduction in ~30-45% of patients and improvement in total symptom scores in 35-40% with good tolerability.
View Article and Find Full Text PDFMalar J
January 2025
Global and Tropical Health Division, Menzies School of Health Research, Charles Darwin University, Darwin, NT, Australia.
Background: In moderate-to-high malaria transmission regions, the World Health Organization recommends intermittent preventive treatment in pregnancy (IPTp) with sulfadoxine-pyrimethamine (SP) alongside insecticide-treated bed nets to reduce the adverse consequences of pregnancy-associated malaria. Due to high-grade Plasmodium falciparum resistance to SP, novel treatment regimens need to be evaluated for IPTp, but these increase pill burden and treatment days. The present qualitative study assessed the acceptability of IPTp-SP plus dihydroartemisinin-piperaquine (DP) in Papua New Guinea, where IPTp-SP was implemented in 2009.
View Article and Find Full Text PDFFundam Clin Pharmacol
February 2025
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62514, Egypt.
Drug repurposing of well-established drugs to be targeted against lung cancer has been a promising strategy. Bosentan is an endothelin 1 (ET-1) blocker widely used in pulmonary hypertension. The current experiment intends to inspect the anticancer and antiangiogenic mechanism of bosentan targeting epidermal growth factor receptor (EGFR) /extra-cellular Signal Regulated Kinase (ERK) /c-Jun/vascular endothelial growth factor (VEGF) carcinogenic pathway.
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