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.

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

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Other information

Language

English

Type of outcome

Prezentace na konferencích

Country of publisher

Czech Republic

Confidentiality degree

není předmětem státního či obchodního tajemství

Organization unit

Faculty of Pharmacy

Tags

ÚChL

Tags

International impact

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Abstract

V originále

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.