2025
Aniline Derivatives as Potent Carbonic Anhydrase Inhibitors
ŠELIGOVÁ, Karolína; Eva HAVRÁNKOVÁ a Jozef CSÖLLEIZákladní údaje
Originální název
Aniline Derivatives as Potent Carbonic Anhydrase Inhibitors
Autoři
Vydání
53rd Conference Synthesis and Analysis of Drugs 2025, 2025
Další údaje
Jazyk
angličtina
Typ výsledku
Prezentace na konferencích
Obor
30104 Pharmacology and pharmacy
Utajení
není předmětem státního či obchodního tajemství
Označené pro přenos do RIV
Ano
Organizační jednotka
Farmaceutická fakulta
ISBN
978-80-280-0773-7
Klíčová slova anglicky
carbonic anhydrase inhibition; triazine; benzenesulfonamide; aniline
Změněno: 18. 11. 2025 11:04, PharmDr. Karolína Šeligová
Anotace
V originále
Carbonic anhydrases are omnipresent metalloenzymes that catalyze reversible conversion of carbon dioxide to bicarbonate and proton, maintaining homeostasis. In humans, they are involved in multiple physiological processes, and they are linked to many disorders, such as glaucoma, neurodegeneration or cancer. Their potential inhibition is of considerable interest in biomedical research. [1]. In bacteria, inhibition of carbonic anhydrases leads to inhibition of their growth and makes them more vulnerable to host defense mechanisms [2]. Based on our previous findings, where a lead 1,3,5-triazinyl aminobenzenesulfonamide incorporating an aniline motif exhibited high inhibitory activity against carbonic anhydrase (Kᵢ = 7.4 nM against CA IX ), we designed and synthesized a series of related derivatives to further explore structure–activity relationships and improve selectivity. The new compounds were evaluated for their inhibitory activity against various CA isoforms.
Návaznosti
| MUNI/A/1474/2024, interní kód MU |
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| MUNI/G/1002/2021, interní kód MU |
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