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Antimicrobial and Antiproliferative Properties of 2-Phenyl-N-(Pyridin-2-yl)acetamides
D. Nawrot, B. Koutníková, O. Janďourek, K. Konečná, M. Novák, P. Paterová, P. Bárta, G. Bouz, J. Zitko, M. Doležal
Jazyk angličtina Země Anglie, Velká Británie
Typ dokumentu časopisecké články
Grantová podpora
SVV 260 666
Ministry of Education, Youth and Sports of the Czech Republic
NU21-05-00482
Ministry of Health of the Czech Republic
PubMed
39835639
DOI
10.1111/cbdd.70030
Knihovny.cz E-zdroje
- MeSH
- acetamidy * chemie farmakologie MeSH
- antifungální látky farmakologie chemie chemická syntéza MeSH
- antituberkulotika farmakologie chemie MeSH
- buňky Hep G2 MeSH
- lidé MeSH
- mikrobiální testy citlivosti * MeSH
- Mycobacterium tuberculosis * účinky léků MeSH
- nádorové buněčné linie MeSH
- proliferace buněk * účinky léků MeSH
- protinádorové látky farmakologie chemie MeSH
- pyridiny chemie farmakologie MeSH
- SARS-CoV-2 účinky léků MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Infectious diseases, including bacterial, fungal, and viral, have once again gained urgency in the drug development pipeline after the recent COVID-19 pandemic. Tuberculosis (TB) is an old infectious disease for which eradication has not yet been successful. Novel agents are required to have potential activity against both drug-sensitive and drug-resistant strains of Mycobacterium tuberculosis (Mtb), the causative agent of TB. In this study, we present a series of 2-phenyl-N-(pyridin-2-yl)acetamides in an attempt to investigate their possible antimycobacterial activity, cytotoxicity on the HepG2 liver cancer cell line, and-as complementary testing-their antibacterial and antifungal properties against a panel of clinically important pathogens. This screening resulted in one compound with promising antimycobacterial activity-compound 12, MICMtb H37Ra = 15.625 μg/mL (56.26 μM). Compounds 17, 24, and 26 were further screened for their antiproliferative activity against human epithelial kidney cancer cell line A498, human prostate cancer cell line PC-3, and human glioblastoma cell line U-87MG, where they were found to possess interesting activity worth further exploration in the future.
Biomedical Research Centre University Hospital Hradec Kralove Hradec Králové Czech Republic
Department of Clinical Microbiology University Hospital Hradec Králové Czech Republic
Faculty of Pharmacy in Hradec Králové Charles University Hradec Králové Czech Republic
Citace poskytuje Crossref.org
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