The Design, Synthesis and Evaluation of Rho-kinase Inhibitory Activity of 4-aryl-thiazole-2-amines
| Author | Linan Wang | en |
| Author | Ben Ouyang | en |
| Author | Meixia Fan | en |
| Author | Junhui Qi | en |
| Author | Lei Yao | en |
| Issued Date | 2021-07-31 | en |
| Abstract | Rho-associated kinases (ROCK) are a class of serine/threonine kinases that play important roles in various biological processes. ROCK are becoming attractive targets for drug designing. A novel scaffold was designed according to molecular hybridization strategy, then a series of 4-aryl-5-aminomethyl-thiazole-2-amines were synthesized, and their inhibitory activities on ROCK were screened by enzyme-linked immunosorbent assay (ELISA). The results showed that 4-aryl-5-aminomethyl-thiazole-2-amines derivatives displayed certain ROCK II inhibitory activities. The IC50 value of the most potent compound 4v was found to be 20 nM. The preliminary structure-activity-relationship investigation showed that compounds with 4-pyridine substitution were generally found to be more potent than compounds with 3-pyridine substitution. The molecular docking studies indicated that more optimization work needs to conduct to obtain more potent ROCK inhibitors. | en |
| DOI | https://doi.org/10.22037/ijpr.2020.114468.14866 | en |
| Keyword | 4-aryl-thiazole-2-amine | en |
| Keyword | Inhibitors | en |
| Keyword | Kinase | en |
| Keyword | ROCK | en |
| Keyword | Synthesis | en |
| Publisher | Brieflands | en |
| Title | The Design, Synthesis and Evaluation of Rho-kinase Inhibitory Activity of 4-aryl-thiazole-2-amines | en |
| Type | Original Article | en |
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