Publication details

NOVEL 1,3,5-TRIAZINYL AMINOBENZENESULFONAMIDES AS POTENT ANTI-VRE AGENTS, AND CARBONIC ANHYDRASES I, II, VII, IX, AND XII INHIBITORS

Authors

HAVRÁNKOVÁ Eva JAMPÍLEK Josef GARAJ Vladimír SUPURAN Claudiu T.

Year of publication 2022
Type Article in Proceedings
Conference Czech Chemical Society Symposium Series
MU Faculty or unit

Faculty of Pharmacy

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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