Document Detail

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    
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.
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.
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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