Triazinyl-substituted benzenesulfonamides as inhibitors of bacterial carbonic anhydrase

HAVRÁNKOVÁ, Eva. Triazinyl-substituted benzenesulfonamides as inhibitors of bacterial carbonic anhydrase. In Conference Synthesis and Analysis of Drugs 2021. 2021.

Základní údaje

• Originální název: Triazinyl-substituted benzenesulfonamides as inhibitors of bacterial carbonic anhydrase
• Název česky: Triazinylem substituované benzensulfonamidy jako inhibitory bakteriálních karboanhydráz
• Autoři: HAVRÁNKOVÁ, Eva.
• Vydání: Conference Synthesis and Analysis of Drugs 2021, 2021.

Další údaje

• Originální jazyk: angličtina
• Typ výsledku: Prezentace na konferencích
• Stát vydavatele: Česká republika
• Utajení: není předmětem státního či obchodního tajemství
• Organizační jednotka: Farmaceutická fakulta
• Štítky: ÚChL
• Příznaky: Mezinárodní význam

Anotace

Carbonic anhydrases (CA, EC 4.2.1.1) are metalloenzymes present in pathogenic bacteria. CAs play an important role in growth and survival in bacteria. Inhibition of bacterial CAs leads to growth retardation, growth defects and makes bacterias vulnerable to host defense mechanisms. Bacterial CAs are therefore a very promising target in the search for new antibiotics. The new 1,3,5-triazinyl aminobenzenesulfonamide derivatives containing aminoalcohole, aminochalcone and other structural moieties were synthesized, and their biological activity was evaluated. Some of the tested compounds exhibit a significant inhibitory activity against vancomycin resistant Enterococcus faecalis, while against relevant human CAs they showed almost negligible inhibitory activity. In conclusion, 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.