Results 1 to 10 of about 1,466 (128)

Potent carbonic anhydrase I, II, IX and XII inhibition activity of novel primary benzenesulfonamides incorporating bis-ureido moieties [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
A novel series of twelve aromatic bis-ureido-substituted benzenesulfonamides was synthesised by conjugation of aromatic aminobenzenesulfonamides with aromatic bis-isocyanates.
Tuba Tekeli, Suleyman Akocak, Andrea Petreni, Nebih Lolak, Servet Çete, Claudiu T. Supuran   +5 more
doaj   +2 more sources

Detailed Studies on the Methoxylation and Subsequent Dealkylation of N,N-Diethylbenzenesulfonamide Using a Tailor-Made Electrosynthetic Reactor [PDF]

Molecules
Benzenesulfonamides are an outstandingly important family of compounds in organic and medicinal chemistry. Herein, we report detailed studies on the electrochemical mono- and dideethylation of model compound N,N-diethylbenzenesulfonamide. In this context,
Ernák F. Várda, Imre Gyűjtő, Ferenc Ender, Richárd Csekő, György T. Balogh, Balázs Volk   +5 more
doaj   +2 more sources

Quantitative Competition Binding of Fluorinated Ligands by Real-Time ¹⁹F In-Cell NMR to Assess Isoform Selectivity in Human Cells. [PDF]

Magn Reson Chem
Real‐time in‐cell 19F NMR spectroscopy in a flow NMR bioreactor was used to monitor the binding of fluorinated compounds to three cytosolic carbonic anhydrase isoforms in living human cells. The simultaneous observation of the two ligands allowed for the quantitative ranking of their intracellular affinities by competition binding. This approach allows
Costantino A, Barbieri L, Giovannuzzi S, Nocentini A, Supuran CT, Luchinat E.   +5 more
europepmc   +2 more sources

HIV nucleocapsid proteins as targets for novel 1,2-benzisothiazol-3(2H)-one benzenesulfonamides: synthesis and antiretroviral activity [PDF]

Frontiers in Microbiology
A new class of 1,2-benzisothiazol-3(2H)-one benzenesulfonamides has been synthesized. In cell-based assays, the lead compound 6 inhibits the replication of HIV-1, HIV-2, and HIV-1 variants carrying clinically relevant mutations against non-nucleoside ...
Roberta Loddo, Matteo Incerti, Elda Favari, Valeria Manca, Marta Cogoni, Rebecca Piras, Luca Virdis, Vanessa Palmas, Elena Tamburini, Paolo La Colla, Giuseppina Sanna   +10 more
doaj   +2 more sources

Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamides as carbonic anhydrase isoforms I and II inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes that are involved in diverse bioprocesses. We report the synthesis and biological evaluation of novel series of benzenesulfonamides incorporating un/substituted ethyl quinoline-3 ...
Mohammad M Al-Sanea, Ahmed Elkamhawy, Silvia Bua   +2 more
exaly   +2 more sources

Benzenesulfonamide derivatives as Vibrio cholerae carbonic anhydrases inhibitors: a computational-aided insight in the structural rigidity-activity relationships [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Vibrio cholerae causes life-threatening infections in low-income countries due to the rise of antibacterial resistance. Innovative pharmacological targets have been investigated and carbonic anhydrases (CAs, EC: 4.2.1.1) encoded by V.
Marialuigia Fantacuzzi, Ilaria D’Agostino, Simone Carradori, Francesco Liguori, Fabrizio Carta, Mariangela Agamennone, Andrea Angeli, Filomena Sannio, Jean-Denis Docquier, Clemente Capasso, Claudiu T. Supuran   +10 more
doaj   +2 more sources

Diversely N-substituted benzenesulfonamides dissimilarly bind to human carbonic anhydrases: crystallographic investigations of N-nitrosulfonamides [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Carbonic anhydrases (CAs) are a zinc metalloenzymes that catalyse the reversible hydration of carbon dioxide to bicarbonate and proton, pivotal for a wide range of biological processes. CAs are involved in numerous pathologies and thus represent valuable
Andrea Angeli, Marta Ferraroni, Alessandro Bonardi, Claudiu T. Supuran, Alessio Nocentini   +4 more
doaj   +2 more sources

4-(3-Alkyl/benzyl-guanidino)benzenesulfonamides as selective carbonic anhydrase VII inhibitors [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
The treatment of chronic neuropathic pain remains one of the most challenging of all neurological diseases and very much an art. There exists no consensus for the optimal management of this condition at the moment. Gaining inspiration from recent studies
Morteza Abdoli, Simone Giovannuzzi, Claudiu T. Supuran, Raivis Žalubovskis   +3 more
doaj   +2 more sources

Design, Synthesis, and Antimicrobial Evaluation of New Thiopyrimidine–Benzenesulfonamide Compounds [PDF]

Molecules
Bacterial infection poses a serious threat to human life due to the rapidly growing resistance of bacteria to antibacterial drugs, which is a significant public health issue.
Abdalrahman Khalifa, Manal M. Anwar, Walaa A. Alshareef, Eman A. El-Gebaly, Samia A. Elseginy, Sameh H. Abdelwahed   +5 more
doaj   +2 more sources

Small-molecule screen in C. elegans identifies benzenesulfonamides as inhibitors of microsporidia spores [PDF]

npj Antimicrobials and Resistance
Microsporidia, a large group of fungal-related intracellular parasites, infect several economically significant animals, leading to substantial economic losses.
Qingyuan Huang, Haiyi Jiang, Junhong Wei, Yabin Dou, Guoqing Pan, Jie Chen, Aaron W. Reinke   +6 more
doaj   +2 more sources