Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma
|dc.contributor.author||Kumar, Alan Prem|
|dc.identifier.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.|
Â© 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 (9aâ€“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 Âµg/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.
|dc.title||Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma|
|dcterms.source.title||Bioorganic & Medicinal Chemistry|
|curtin.department||Curtin Medical School|
|curtin.accessStatus||Fulltext not available|
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