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  • Pyrimido[1,2-b]indazole derivatives : selective inhibitors of human monoamine oxidase B with neuroprotective activity
    Jismy, Badr ...
    Structurally diverse heterotricyclic compounds are recognized as monoamine oxidase (MAO) inhibitors and thus represent an appealing scaffold in development and optimization of novel MAO inhibitors. ... Herein we explored the chemical space of pyrimido[1,2-b]indazoles as MAO inhibitors by preparing a small library of (hetero)aryl derivatives. An efficient synthetic strategy was developed starting from commercially available 1H-indazol-3-amines, which were converted to various 3-bromoheterotricyclic derivatives and further functionalized via Suzuki-Miyaura coupling reaction. Derivatives 4a-t selectively inhibited human MAO-B isoform in a reversible and competitive manner as confirmed by kinetic experiments and docking studies. Selected derivatives were not cytotoxic to neuroblastoma SH-SY5Y cells. Moreover, analogue 4i protected human neuroblastoma SH-SY5Y cells against 6-hydroxydopamine-induced cell death, which confirms the applicability of the pyrimido[1,2-b]indazoles as potential antiparkinsonian agents.
    Vir: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 209, 2021, str. 1-16)
    Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasle
    Leto - 2021
    Jezik - angleški
    COBISS.SI-ID - 31851523

    Povezava(-e):

    https://www.sciencedirect.com/science/article/pii/S0223523420308837#!
    DOI

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