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  • Synthesis and biological assessment of racemic benzochromenopyrimidinimines as antioxidant, cholinesterase, and $▫ [Aß1-42]▫$ aggregation Inhibitors for Alzheimer's disease therapy
    Dgachi, Youssef ...
    Given the complex nature of Alzheimer's disease (AD), compounds that are able to simultaneously address two or more AD-associated targets show greater promise for development into drugs for AD ... therapy. Herein we report an efficient two-step synthesis and biological evaluation of new racemic benzochromene derivatives as antioxidants, inhibitors of cholinesterase and ß-amyloid (Aß 41) aggregation. Based on the results of the primary screening, we identified 15-(3-methoxyphenyl)-9,11,12,15-tetrahydro-10H,14H-benzo[5,6]chromeno[2,3-d]pyrido[1,2-a]pyrimidin-14-imine (3e) and 16-(3-methoxyphenyl)-9,10,11,12,13,16-hexahydro-15H-benzo[5,6]chromeno[2,3, 4]pyrimido[1,2-a]azepin-15-imine (3f) as new potential multitarget-directed ligands for AD therapy. Further in-depth biological analysis showed that compound 3f is a good human acetylcholinesterase inhibitor [IC50=(0.36-0.02)microm], has strong antioxidant activity (3.61micromol Trolox equivalents), and moderate Aß41-42 antiaggregating power (40.3%).
    Source: ChemMedChem : Chemistry Enabling Drug Discovery. - ISSN 1860-7179 (Vol. 11, iss. 12, 2016, str. 1318-1327)
    Type of material - e-article
    Publish date - 2016
    Language - english
    COBISS.SI-ID - 4022897

    Link(s):

    http://onlinelibrary.wiley.com/doi/10.1002/cmdc.201500539/abstract

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