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Fakulteta za farmacijo, Ljubljana (FFALJ)
  • Indoles and 1-(3-(benzyloxy)benzyl)piperazines : reversible and selective monoamine oxidase B inhibitors identified by screening an in-house compound library
    Knez, Damijan, farmacevt ...
    The therapeutic indications for monoamine oxidases A and B (MAO-A and MAO-B) inhibitors that have emerged from biological studies on animal and cellular models of neurological and oncological ... diseases have focused drug discovery projects upon identifying reversible MAO inhibitors. Screening of our in-house academic compound library identified two hit compounds that inhibit MAO-B with IC50 values in micromolar range. Two series of indole (23 analogues) and 3-(benzyloxy)benzyl)piperazine (16 analogues) MAO-B inhibitors were derived from hits, and screened for their structure-activity relationships. Both series yielded low micromolar selective inhibitors of human MAO-B, namely indole 2 (IC50 = 12.63 ± 1.21 µM) and piperazine 39 (IC50 = 19.25 ± 4.89 µM), which is comparable to selective MAO-B inhibitor isatin (IC50 = 6.10 ± 2.81 µM), yet less potent in comparison to safinamide (IC50 = 0.029 ± 0.002 µM). Selective MAO-B inhibitors 2, 14, 38 and 39 exhibited favourable permeation of the blood-brain barrier and low cytotoxicity in the human neuroblastoma cell line SH-SY5Y.
    Vir: Bioorganic chemistry. - ISSN 0045-2068 (Vol. 119, 2022, str. 1-19)
    Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasle
    Leto - 2022
    Jezik - angleški
    COBISS.SI-ID - 91639299

    Povezava(-e):

    https://www.sciencedirect.com/science/article/pii/S0045206821009597
    DOI

vir: Bioorganic chemistry. - ISSN 0045-2068 (Vol. 119, 2022, str. 1-19)

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