Document Detail


Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives.
MedLine Citation:
PMID:  14998586     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A novel series of tetrahydrothieno[2,3-h]cinnolinone derivatives were synthesized and evaluated in vitro for their ability to inhibit aldose reductase (ALR2), an enzyme involved in the appearance of diabetic complications. Compounds 2e and 2j exert a remarkable inhibitory effect, with IC(50) of 7.6 and 18 microM, respectively. These compounds incorporate a valid pharmacophore for aldose reductase inhibitory activity represented by a thienocinnolinone template linked through a pentamethylene spacer to a carboxylic function.
Authors:
A Pau; B Asproni; G Boatto; G E Grella; P De Caprariis; L Costantino; G A Pinna
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences     Volume:  21     ISSN:  0928-0987     ISO Abbreviation:  Eur J Pharm Sci     Publication Date:  2004 Mar 
Date Detail:
Created Date:  2004-03-04     Completed Date:  2004-11-04     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9317982     Medline TA:  Eur J Pharm Sci     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  545-52     Citation Subset:  IM    
Affiliation:
Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, Via Muroni 23/A, 07100 Sassari, Italy. pau@ssmain.uniss.it
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MeSH Terms
Descriptor/Qualifier:
Aldehyde Reductase / antagonists & inhibitors*,  metabolism
Animals
Carboxylic Acids / chemical synthesis*,  pharmacology
Enzyme Inhibitors / chemical synthesis*,  pharmacology
Swine
Thiophenes / chemical synthesis*,  pharmacology
Chemical
Reg. No./Substance:
0/Carboxylic Acids; 0/Enzyme Inhibitors; 0/Thiophenes; EC 1.1.1.21/Aldehyde Reductase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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