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Iran J Pharm Res. 2021;20(3):121-131. doi: 10.22037/ijpr.2020.114468.14866.

The Design, Synthesis and Evaluation of Rho-kinase Inhibitory Activity of 4-aryl-thiazole-2-amines.

Iranian journal of pharmaceutical research : IJPR

Linan Wang, Ben Ouyang, Meixia Fan, Junhui Qi, Lei Yao

Affiliations

  1. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264003, China.

PMID: 34903975 PMCID: PMC8653655 DOI: 10.22037/ijpr.2020.114468.14866

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 IC

Keywords: 4-aryl-thiazole-2-amine; Inhibitors; Kinase; ROCK; Synthesis

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