| Structure-activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors. | |
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MedLine Citation:
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PMID: 21733683 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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A series of α-glutamic acid scaffold based 4-(benzamido)-4-(1,3,4-oxadiazol-2-yl) butanoic acids were designed and synthesized as new ADAMTS inhibitors. The compounds dose-dependently inhibited the enzymatic activities of ADAMTS-4 and ADAMTS-5. One of the most active compound 2h potently inhibited ADAMTS-4 and ADAMTS-5 with IC(50) values of 1.2 and 0.8μM, respectively. These inhibitors may serve as new lead compounds for further development of therapeutics to treat osteoarthritis. |
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Authors:
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Lijie Peng; Lei Duan; Xiaofeng Liu; Mengjie Shen; Yingjun Li; Jiajie Yan; Honglin Li; Ke Ding |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-6-16 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2011 Jun |
Date Detail:
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Created Date: 2011-7-7 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier Ltd. All rights reserved. |
Affiliation:
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Key Laboratory of Regenerative Biology, Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, No. 190, Kaiyuan Avenue, Science Park, Guangzhou 510530, China; Graduate School of Chinese Academy of Sciences, #19 Yuquan Road, Beijing 100049, China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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