Document Detail


Synthesis of 1,2,4-triazole derivatives: binding properties on endothelin receptors.
MedLine Citation:
PMID:  18045205     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In the present study we describe the synthesis of a new series of 1,2,4-triazoles: [3-(arylmethyl)thio-5-aryl-4H-[1,2,4]triazol-4-yl]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-yl]acetic acids 8a-d, and [3-(aryl-methyl)thio-5-aryl-1H-[1,2,4]triazol-1-yl] acetic acids 9a-d. These compounds were tested in binding assays to evaluate their ability as ligands for human ET(A) and ET(B) receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.
Authors:
L Salerno; F Guerrera; M Modica; G Romeo; V Pittalà; M A Siracusa; I Mereghetti; A Cagnotto; T Mennini
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Medicinal chemistry (Shāriqah (United Arab Emirates))     Volume:  3     ISSN:  1573-4064     ISO Abbreviation:  -     Publication Date:  2007 Nov 
Date Detail:
Created Date:  2007-11-29     Completed Date:  2007-12-19     Revised Date:  2008-02-26    
Medline Journal Info:
Nlm Unique ID:  101240303     Medline TA:  Med Chem     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  551-60     Citation Subset:  IM    
Affiliation:
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Catania, viale A. Doria, 6, 95125 Catania, Italy. l.salerno@unict.it
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MeSH Terms
Descriptor/Qualifier:
Animals
CHO Cells
Cricetinae
Cricetulus
Humans
Ligands
Protein Binding
Receptor, Endothelin A / genetics,  metabolism
Receptor, Endothelin B / genetics,  metabolism
Receptors, Endothelin / genetics,  metabolism*
Structure-Activity Relationship
Transfection
Triazoles / chemical synthesis*,  pharmacology
Chemical
Reg. No./Substance:
0/Ligands; 0/Receptor, Endothelin A; 0/Receptor, Endothelin B; 0/Receptors, Endothelin; 0/Triazoles

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


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