Novel thiazole-thiophene conjugates as adenosine receptor antagonists: synthesis, biological evaluation and docking studies.
Bioorg Med Chem Lett
; 25(6): 1306-9, 2015 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-25686851
ABSTRACT
Here we report novel thiazole-thiophene conjugates as adenosine receptor antagonists. All the molecules were evaluated for their binding affinity for adenosine receptors. Most of the molecules were found to interact with the A1, A2A and A3 adenosine receptor subtypes with good affinity values. The most potent and selective compound 8n showed an A3Ki value of 0.33µM with selectivity ratios of >90 versus the A1 and >30 versus the A2 subtypes. For compound 8n docking studies into the binding site of the A3 adenosine receptor are provided to visualize its binding mode.
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1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiazóis
/
Tiofenos
/
Receptores Purinérgicos P1
/
Antagonistas de Receptores Purinérgicos P1
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article