Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma
© 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 inhibi...
| Main Authors: | , , , , , |
|---|---|
| Format: | Journal Article |
| Published: |
Pergamon
2017
|
| Online Access: | http://hdl.handle.net/20.500.11937/73263 |
| _version_ | 1848762967996235776 |
|---|---|
| author | Abbhi, V. Saini, L. Mishra, S. Sethi, G. Kumar, Alan Prem Piplani, P. |
| author_facet | Abbhi, V. Saini, L. Mishra, S. Sethi, G. Kumar, Alan Prem Piplani, P. |
| author_sort | Abbhi, V. |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | © 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. |
| first_indexed | 2025-11-14T10:55:59Z |
| format | Journal Article |
| id | curtin-20.500.11937-73263 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T10:55:59Z |
| publishDate | 2017 |
| publisher | Pergamon |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-732632018-12-13T09:35:32Z Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma Abbhi, V. Saini, L. Mishra, S. Sethi, G. Kumar, Alan Prem Piplani, P. © 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. 2017 Journal Article http://hdl.handle.net/20.500.11937/73263 10.1016/j.bmc.2017.09.045 Pergamon restricted |
| spellingShingle | Abbhi, V. Saini, L. Mishra, S. Sethi, G. Kumar, Alan Prem Piplani, P. Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma |
| title | Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma |
| title_full | Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma |
| title_fullStr | Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma |
| title_full_unstemmed | Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma |
| title_short | Design and synthesis of benzimidazole-based Rho kinase inhibitors for the treatment of glaucoma |
| title_sort | design and synthesis of benzimidazole-based rho kinase inhibitors for the treatment of glaucoma |
| url | http://hdl.handle.net/20.500.11937/73263 |