SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES
AS POTENTIAL THERAPEUTIC AGENTS

k 2025

SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS

MURGAŠOVÁ, Veronika a Oldřich FARSA

Základní údaje

Originální název

SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS

Autoři

MURGAŠOVÁ, Veronika a Oldřich FARSA

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

schiff bases; basic acetophenone derivative; metalloenzyme inhibitor

Změněno: 5. 1. 2026 14:39, Mgr. Veronika Murgašová

Anotace

V originále

Schiff bases are versatile ligands widely used in metal coordination chemistry, capable of forming stable complexes with a broad range of metal ions. These complexes exhibit extensive therapeutic potential, including antibacterial, antifungal, antiviral, antimalarial, anti-inflammatory, cytotoxic, enzyme-inhibitory, and anticancer properties. Due to their ability to form such complexes, many Schiff bases also serve as important intermediates in various enzymatic reactions. One potential target enzyme is aminopeptidase N (AP-N), a neutral zinc-binding metalloenzyme. Inhibitors of this ubiquitous enzyme may offer broad-spectrum therapeutic applications. Both AP-N and the nuclear factor kappa-B (NF-κB) are critical components involved in various cellular processes. The series of basic thiosemicarbazone, semicarbazone, and hydroxylamine derivatives of acetophenone with diverse substitution of various symmetrical secondary amines and heterocyclic amines, were synthesized. Compounds showing the most potent inhibitory activity against AP-N (based on IC50 values) were further tested for their ability to inhibit cell proliferation in three different cell lines. These lead compounds are now also being tested for their potential to inhibit the proinflammatory transcription factor NF-κB, in an effort to uncover deeper connections between AP-N inhibition and inflammation-related signaling pathways.

Návaznosti

MUNI/A/1496/2024, interní kód MU

Název: Syntéza a stanovení biologické účinnosti derivátů ketiminů a jejich inhibiční aktivity na metaloenzymy, a též dalších aktivit na pokročilých biologických systémech

Investor: Masarykova univerzita, Syntéza a stanovení biologické účinnosti derivátů ketiminů a jejich inhibiční aktivity na metaloenzymy, a též dalších aktivit na pokročilých biologických systémech

Citovat

MURGAŠOVÁ, Veronika a Oldřich FARSA. SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS. In 53rd Conference Synthesis and Analysis of Drugs 2025. 2025. ISBN 978-80-280-0773-7.

@proceedings{2544139,
   author = {Murgašová, Veronika and Farsa, Oldřich},
   booktitle = {53rd Conference Synthesis and Analysis of Drugs 2025},
   keywords = {schiff bases; basic acetophenone derivative; metalloenzyme inhibitor},
   language = {eng},
   isbn = {978-80-280-0773-7},
   title = {SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS},
   year = {2025}
}

TY  - CONF
ID  - 2544139
AU  - Murgašová, Veronika - Farsa, Oldřich
PY  - 2025
TI  - SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS
SN  - 9788028007737
KW  - schiff bases
KW  - basic acetophenone derivative
KW  - metalloenzyme inhibitor
N2  - Schiff bases are versatile ligands widely used in metal coordination chemistry, capable of forming stable complexes with a broad range of metal ions. These complexes exhibit extensive therapeutic potential, including antibacterial, antifungal, antiviral, antimalarial, anti-inflammatory, cytotoxic, enzyme-inhibitory, and anticancer properties. Due to their ability to form such complexes, many Schiff bases also serve as important intermediates in various enzymatic reactions. One potential target enzyme is aminopeptidase N (AP-N), a neutral zinc-binding metalloenzyme. Inhibitors of this ubiquitous enzyme may offer broad-spectrum therapeutic applications. Both AP-N and the nuclear factor kappa-B (NF-κB) are critical components involved in various cellular processes. The series of basic thiosemicarbazone, semicarbazone, and hydroxylamine derivatives of acetophenone with diverse substitution of various symmetrical secondary amines and heterocyclic amines, were synthesized. Compounds showing the most potent inhibitory activity against AP-N (based on IC50 values) were further tested for their ability to inhibit cell proliferation in three different cell lines. These lead compounds are now also being tested for their potential to inhibit the proinflammatory transcription factor NF-κB, in an effort to uncover deeper connections between AP-N inhibition and inflammation-related signaling pathways.
ER  -

MURGAŠOVÁ, Veronika a Oldřich FARSA. SYNTHESIS AND EVALUATION OF AMINOACETOPHENONE-DERIVED KETIMINES AS POTENTIAL THERAPEUTIC AGENTS. In \textit{53rd Conference Synthesis and Analysis of Drugs 2025}. 2025. ISBN~978-80-280-0773-7.

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