Design, synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors. Issue 19 (1st October 2020)

• Record Type: Journal Article
• Authors: Ma, Shuchao; Wang, Linan; Ouyang, Ben; Fan, Meixia; Qi, Junhui; Yao, Lei
• Is Part Of: Bioorganic & medicinal chemistry. Volume 28:Issue 19(2020)
• Publication Date: 2020-10-01
• Subjects: ROCK -- Inhibitors -- 4-Aryl-5-aminoalkyl-thiazole-2-amines -- Synthesis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2020.115683
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: A series of 4-aryl-5-aminoalkyl-thiazole-2-amines were designed, synthesized, and their inhibitory activity on ROCK II was screened by enzyme-linked immunosorbent assay (ELISA). Compound 10l showed ROCK II inhibitory activity with IC50 value of 20 nM. Abstract: A series of 4-aryl-5-aminoalkyl-thiazole-2-amines were designed and synthesized, and their inhibitory activity on ROCK II was screened by enzyme-linked immunosorbent assay (ELISA). The results showed that 4-aryl-5-aminomethyl-thiazole-2-amines derivatives had certain ROCK II inhibitory activities. Compound 10l showed ROCK II inhibitory activity with IC50 value of 20 nM.