Počet záznamů: 1  

Trifluoromethylcinnamanilide Michael Acceptors for Treatment of Resistant Bacterial Infections

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    SYSNO ASEP0566362
    Druh ASEPJ - Článek v odborném periodiku
    Zařazení RIVJ - Článek v odborném periodiku
    Poddruh JČlánek ve WOS
    NázevTrifluoromethylcinnamanilide Michael Acceptors for Treatment of Resistant Bacterial Infections
    Tvůrce(i) Strharsky, T. (CZ)
    Pindjakova, D. (SK)
    Kos, J. (SK)
    Vrablova, L. (SK)
    Smak, P. (CZ)
    Michnová, H. (CZ)
    Gonec, T. (CZ)
    Hošek, J. (CZ)
    Oravec, Michal (UEK-B) RID, ORCID, SAI
    Jendrzejewska, I. (PL)
    Čížek, A. (CZ)
    Jampílek, J. (SK)
    Celkový počet autorů12
    Číslo článku15090
    Zdroj.dok.International Journal of Molecular Sciences. - : MDPI
    Roč. 23, č. 23 (2022)
    Poč.str.22 s.
    Jazyk dok.eng - angličtina
    Země vyd.CH - Švýcarsko
    Klíč. slovacinnamamides ; Michael acceptors ; antimicrobial activity ; cytotoxicity ; lipophilicity ; structure-activity relationships ; docking study
    Vědní obor RIVCE - Biochemie
    Obor OECDBiochemistry and molecular biology
    CEPLM2018123 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy
    EF16_019/0000797 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy
    Způsob publikováníOpen access
    Institucionální podporaUEK-B - RVO:86652079
    UT WOS000897240400001
    EID SCOPUS85143746002
    DOI10.3390/ijms232315090
    AnotaceA series of thirty-two anilides of 3-(trifluoromethyl)cinnamic acid (series 1) and 4-(trifluoromethyl)cinnamic acid (series 2) was prepared by microwave-assisted synthesis. All the compounds were tested against reference strains Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 and resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant E. faecalis (VRE). All the compounds were evaluated in vitro against Mycobacterium smegmatis ATCC 700084 and M. marinum CAMP 5644. (2E)-3-[3-(Trifluoromethyl)phenyl]-N-[4-(trifluoromethyl)phenyl]prop-2-enamide (1j), (2E)-N-(3,5-dichlorophenyl)-3-[3-(trifluoromethyl)phenyl]prop-2-enamide (1o) and (2E)-N-[3-(trifluoromethyl)phenyl]-3-[4-(trifluoromethyl)-phenyl]prop-2-enamide (2i), (2E)-N-[3,5-bis(trifluoromethyl)phenyl]-3-[4-(trifluoromethyl)phenyl]-prop-2-enamide (2p) showed antistaphylococcal (MICs/MBCs 0.15-5.57 mu M) as well as anti-enterococcal (MICs/MBCs 2.34-44.5 mu M) activity. The growth of M. marinum was strongly inhibited by compounds 1j and 2p in a MIC range from 0.29 to 2.34 mu M, while all the agents of series 1 showed activity against M. smegnatis (MICs ranged from 9.36 to 51.7 mu M). The performed docking study demonstrated the ability of the compounds to bind to the active site of the mycobacterial enzyme InhA. The compounds had a significant effect on the inhibition of bacterial respiration, as demonstrated by the MTT assay. The compounds showed not only bacteriostatic activity but also bactericidal activity. Preliminary in vitro cytotoxicity screening was assessed using the human monocytic leukemia cell line THP-1 and, except for compound 2p, all effective agents did show insignificant cytotoxic effect. Compound 2p is an interesting anti-invasive agent with dual (cytotoxic and antibacterial) activity, while compounds 1j and 1o are the most interesting purely antibacterial compounds within the prepared molecules.
    PracovištěÚstav výzkumu globální změny
    KontaktNikola Šviková, svikova.n@czechglobe.cz, Tel.: 511 192 268
    Rok sběru2023
    Elektronická adresahttps://www.mdpi.com/1422-0067/23/23/15090
Počet záznamů: 1  

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