%0 Journal Article
%T Synthesis of a new series of 3-functionalised-1-phenyl-1,2,3-triazole sulfamoylbenzamides as carbonic anhydrase I, II, IV and IX inhibitors
%A Andrea Angeli
%A Baijayantimala Swain
%A Claudiu T. Supuran
%A Mohammed Arifuddin
%A Pavitra S. Thacker
%A Priti Singh
%A Srinivas Angapelly
%J Journal of Enzyme Inhibition and Medicinal Chemistry
%D 2019
%R https://doi.org/10.1080/14756366.2019.1629432
%X Abstract The synthesis of a novel series of 3-functionalised benzenesulfonamides incorporating phenyl-1,2,3-triazole with an amide linker was achieved by using the ¡°click-tail¡± approach. The new compounds, including the intermediates, were assayed as inhibitors of human carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I and II (cytosolic isoforms) and also for hCA IV and IX (transmembrane isoforms) taking acetazolamide as standard drug. Most of these compounds exhibited excellent activity against all these isoforms. hCA I was inhibited with Kis in the range of 50.8¨C966.8£¿nM, while the glaucoma associated hCA II was inhibited with Kis in the range of 6.5¨C760.0£¿nM. Isoform hCA IV was inhibited with Kis in the range of 65.3¨C957.5£¿nM, whereas the tumor associated hypoxia induced hCA IX was inhibited with Kis in the range of 30.8¨C815.9£¿nM. The structure activity relationship study for the 3-functionalised-1-phenyl-1,2,3-triazole sulfamoylbenzamides against these isoforms was also inferred from the results
%U https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1629432