Document Detail

Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase.
MedLine Citation:
PMID:  19758809     Owner:  NLM     Status:  MEDLINE    
A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. The structure-activity relationships (SAR) of these compounds were also presented. Among these, compounds 12, 13l, 13q, and 13v showed moderate activities towards both GK and GP. Compound 13h inhibited hLGP with an IC(50) of 8.95 microM and activated GK with an EC(50) of 1.87 microM. The possible binding modes of compounds 12, 13l, 13h, and 13q with GP and GK were also explored by molecular docking simulation.
Lei Zhang; Honglin Li; Qingzhang Zhu; Jun Liu; Ling Chen; Ying Leng; Hualiang Jiang; Hong Liu
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-08-24
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  17     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2009 Oct 
Date Detail:
Created Date:  2009-10-06     Completed Date:  2010-01-19     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  7301-12     Citation Subset:  IM    
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR China.
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MeSH Terms
Benzamides / chemistry,  pharmacology*
Enzyme Activation
Glucokinase / metabolism*
Glycogen Phosphorylase / antagonists & inhibitors*
Hypoglycemic Agents / chemistry,  pharmacology*
Structure-Activity Relationship
Reg. No./Substance:
0/Benzamides; 0/Hypoglycemic Agents; 27208-38-4/benzamide; EC 2.4.1.-/Glycogen Phosphorylase; EC

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