Informace o publikaci

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

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HAVRÁNKOVÁ Eva JAMPÍLEK Josef GARAJ Vladimír SUPURAN Claudiu T.

Rok publikování 2022
Druh Článek ve sborníku
Konference Czech Chemical Society Symposium Series
Fakulta / Pracoviště MU

Farmaceutická fakulta

Citace
www http://www.ccsss.cz/index.php/ccsss/issue/view/31/45
Klíčová slova carbonic anhydrases; vancomycin-resistant enterococci; anti-VRE agents; triazinyl-benzenesulfonamides
Popis 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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