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Structure-activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors.
MedLine Citation:
PMID:  21733683     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
Lijie Peng; Lei Duan; Xiaofeng Liu; Mengjie Shen; Yingjun Li; Jiajie Yan; Honglin Li; Ke Ding
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-6-16
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-7-7     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
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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