Design,synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors |
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| Affiliation: | 1. School of Chemical and Environmental Engineering, Shanghai Institute of Technology, 100 Hai Quan Rd, Shanghai 201418, PR China;2. Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Ling Ling Rd, Shanghai 200032, PR China;3. Medicinal Chemistry, Translational Research Institute, The Scripps Research Institute, Florida, Jupiter, FL 33458, USA;1. Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, 605 Fenglin Road, Nanchang, Jiangxi 330013, China;2. College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang, Jiangxi 330004, China;1. School of Medicine, Zhejiang University City College, Hangzhou 310015, PR China;2. Zhejiang Province Key Laboratory of Anti-Cancer Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China;1. Department of Chemistry, Marquette University, P. O. Box 1881, Milwaukee, WI 53201-1881, United States;2. School of Pharmacy, Center for Structure-based Drug Design and Development, Concordia University Wisconsin, Mequon, WI 53097, United States;1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Material Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;2. The State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Material Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;1. College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea;2. Infectious Disease Research Center, Korea Research Institute of Chemical Technology (KRICT), Daejeon 34114, Republic of Korea;3. Graduate School of New Drug Discovery and Development, Chungnam National University, Daejeon 34134, Republic of Korea |
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| 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. |
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| Keywords: | ROCK Inhibitors 4-Aryl-5-aminoalkyl-thiazole-2-amines Synthesis |
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