Design, synthesis, SAR, and biological evaluation of saccharin‐based hybrids as carbonic anhydrase inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200019
Abstract: Saccharin is a cyclic secondary sulfonamide, which is a selective inhibitor of the tumor‐associated carbonic anhydrase (CA; EC 4.2.1.1) enzymes CA IX and CA XII compared to many primary sulfonamides. In this study, new saccharin‐1,2,3‐triazole… read more here.
Keywords: design synthesis; carbonic anhydrase; hca; hca hca ... See more keywords
Discovery of potent anti-convulsant carbonic anhydrase inhibitors: Design, synthesis, in vitro and in vivo appraisal.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.07.019
Abstract: We report the design, synthesis and pharmacological assessment of novel benzenesulfonamide derivatives acting as effective carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. All the synthesized compounds were screened for their CA inhibitory action against four isoforms… read more here.
Keywords: design synthesis; anhydrase inhibitors; carbonic anhydrase; hca ... See more keywords
Investigation of the inhibitory effects of isoindoline-1,3-dion derivatives on hCA-I and hCA-II enzyme activities
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Molecular Structure"
DOI: 10.1016/j.molstruc.2019.07.070
Abstract: Abstract Inhibition of carbonic anhydrase (CA) has emerged as a promising approach for the treatment of a variety of diseases such as glaucoma, epilepsy, obesity and cancer. As a result, the design of CA inhibitors… read more here.
Keywords: investigation inhibitory; inhibitory effects; isoindoline dion; effects isoindoline ... See more keywords
Carbonic anhydrase inhibition with a series of novel benzenesulfonamide-triazole conjugates
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2018.1513927
Abstract: Abstract We report the synthesis and characterisation of a novel series of triazole benzenesulfonamide derivatives, which incorporate the general pharmacophore associated with carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The synthesised compounds were tested in vitro… read more here.
Keywords: carbonic anhydrase; inhibition; series; hca hca ... See more keywords
S-substituted 2-mercaptoquinazolin-4(3H)-one and 4-ethylbenzensulfonamides act as potent and selective human carbonic anhydrase IX and XII inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2020.1742117
Abstract: Abstract We evaluated the hCA (CA, EC 4.2.1.1) inhibitory activity of novel 4-(2-(2-substituted-thio-4-oxoquinazolin-3(4H)-yl)ethyl)benzenesulfonamides (compounds 2–20) towards the isoforms I, II, IX, and XII. hCA Isoforms were effectively inhibited by most of new compounds comparable to… read more here.
Keywords: hca selectivity; hca xii; hca; selective hca ... See more keywords
Potent carbonic anhydrase I, II, IX and XII inhibition activity of novel primary benzenesulfonamides incorporating bis-ureido moieties
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2023.2185762
Abstract: Abstract A novel series of twelve aromatic bis-ureido-substituted benzenesulfonamides was synthesised by conjugation of aromatic aminobenzenesulfonamides with aromatic bis-isocyanates. The obtained bis-ureido-substituted derivatives were tested against four selected human carbonic anhydrase isoforms (hCA I, hCA… read more here.
Keywords: xii; inhibition; bis ureido; hca ... See more keywords