HAVRÁNKOVÁ, Eva. Triazinyl-substituted benzenesulfonamides as inhibitors of bacterial carbonic anhydrase. In Conference Synthesis and Analysis of Drugs 2021. 2021.
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Basic information
Original name Triazinyl-substituted benzenesulfonamides as inhibitors of bacterial carbonic anhydrase
Name in Czech Triazinylem substituované benzensulfonamidy jako inhibitory bakteriálních karboanhydráz
Authors HAVRÁNKOVÁ, Eva.
Edition Conference Synthesis and Analysis of Drugs 2021, 2021.
Other information
Original language English
Type of outcome Presentations at conferences
Country of publisher Czech Republic
Confidentiality degree is not subject to a state or trade secret
Organization unit Faculty of Pharmacy
Tags ÚChL
Tags International impact
Changed by Changed by: JUDr. Sabina Krejčiříková, učo 383857. Changed: 14/4/2022 14:54.
Abstract
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.
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