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NOVEL 1,3,5-TRIAZINYL AMINOBENZENESULFONAMIDES AS POTENT ANTI-VRE AGENTS, AND CARBONIC ANHYDRASES I, II, VII, IX, AND XII INHIBITORS
Authors | |
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Year of publication | 2022 |
Type | Article in Proceedings |
Conference | Czech Chemical Society Symposium Series |
MU Faculty or unit | |
Citation | |
web | http://www.ccsss.cz/index.php/ccsss/issue/view/31/45 |
Keywords | carbonic anhydrases; vancomycin-resistant enterococci; anti-VRE agents; triazinyl-benzenesulfonamides |
Description | Carbonic anhydrases (CA, EC 4.2.1.1) are metallo-enzymes present in various organisms. In pathogenic bacteria, CAs play an important role in growth and survival. Inhibition of bacterial CAs leads to growth defects, growth retardation and makes bacterias vulnerable to host defense mechanisms. Bacterial CAs are therefore a very promising target in the search for new antibiotics. A series of 1,3,5-triazinyl aminobenzenesulfonamides substituted by aminoalcohol, aminostilbene, and aminochalcone structural motifs were synthesized as potential bacterial CAs inhibitors. Newly prepared compounds have a great potential as antibacterial agents with high activity and at the same time with high selectivity for bacterial CA in comparison with metabolically important hCA isoenzymes (e.g. hCA I, hCA II) found in the human body. |
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