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    Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma

    Access Status
    Fulltext not available
    Authors
    Abbhi, V.
    Saini, L.
    Mishra, S.
    Sethi, G.
    Kumar, Alan Prem
    Piplani, P.
    Date
    2017
    Type
    Journal Article
    
    Metadata
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    Citation
    Abbhi, V. and Saini, L. and Mishra, S. and Sethi, G. and Kumar, A.P. and Piplani, P. 2017. Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma. Bioorganic & Medicinal Chemistry. 25 (21): pp. 6071-6085.
    Source Title
    Bioorganic & Medicinal Chemistry
    DOI
    10.1016/j.bmc.2017.09.045
    ISSN
    0968-0896
    School
    Curtin Medical School
    URI
    http://hdl.handle.net/20.500.11937/73263
    Collection
    • Curtin Research Publications
    Abstract

    © 2017 Rho kinase inhibitors (ROCK II) play a key role in glaucoma management attributed to their IOP lowering ability and neuroprotective effects. In the present study, a series of novel benzimidazole derivatives (9a–m) has been synthesized and evaluated for their IOP lowering, Rho kinase inhibitory and antioxidant properties. The synthesized compounds were found to be lipophilic and showed a significant IOP lowering effect both in the treated and the contralateral eye comparable to the reference standard fasudil. The nitrophenyl piperazine substituted compound 9j exhibited significant IOP lowering (51.56%) and an inhibition of 57.25 and 77.92% towards ROCK II enzyme at a concentration of 0.5 and 1 mM respectively. It possessed a considerable free radical scavenging activity exhibiting an IC50value of 95.49 µg/mL in DPPH assay. The molecular docking studies of compound 9j indicated the binding of the compound at the active site of recombinant human ROCK II which makes it a promising antiglaucoma agent.

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