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- W4307721266 abstract "A one-pot two-step protocol was developed for the synthesis of a series of novel 4-cyanamidobenzenesulfonamides from easily accessible methyl (4-sulfamoylphenyl)-carbamimidothioate. The new sulphonamides were investigated as inhibitors of the enzyme carbonic anhydrase (CA, EC 4.2.1.1), the human (h) cytosolic isoforms hCA I, II, VII, and XIII, as well as three bacterial enzymes belonging to the β-CA class, MscCA from Mammaliicoccus (Staphylococcus) sciuri and StCA1 and StCA2, from Salmonella enterica (serovar Typhimurium). The human isoforms were generally effectively inhibited by these compounds, with a clear structure-activity relationship privileging long aliphatic chains (C6, C7 and C18) as substituents at the cyanamide functionality. The bacterial CAs were also inhibited by these compounds, but not as effective as the hCAs. The most sensitive enzyme to these inhibitors was StCA1 (KIs of 50.7 − 91.1 nM) whereas SscCA was inhibited in the micromolar range (KIs of 0.86–9.59 µM)." @default.
- W4307721266 created "2022-11-05" @default.
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- W4307721266 creator A5035013697 @default.
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- W4307721266 date "2022-10-28" @default.
- W4307721266 modified "2023-09-25" @default.
- W4307721266 title "4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors" @default.
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- W4307721266 doi "https://doi.org/10.1080/14756366.2022.2138367" @default.
- W4307721266 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36305288" @default.
- W4307721266 hasPublicationYear "2022" @default.
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