Synthesis of 11-aryl-5H-imidazo[2,1-c][1,4]benzodiazepines and their benzodiazepine and A1 adenosine binding activity.
Farmaco
; 56(10): 771-8, 2001 Oct.
Article
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| MEDLINE
| ID: mdl-11718270
In the context of a research program aimed at elucidating the properties of the 5H-imidazo[2,1-c][1.4]benzodiazepine system, a series of 11-aryl-5H-imidazo[2,1-c][1,4]benzodiazepines (3a-i) and their 10,11-dihydro-derivatives (4a-i) has been synthesized. The synthetic strategy includes the preparation of the aryl-[1-(2-nitrobenzyl)-1H-imidazol-2-yl]methanones (5a-i) followed by their reduction and subsequent cyclization. Affinities of compounds 3a-i and 4a-i for central benzodiazepine as well as for adenosine A1-receptors were determined by radioligand binding assays. Among the unsaturated analogues, the highest activity at both receptors is displayed by 1H-(2-thienyl) derivative 3e. The hydrogenated analogues 4a-i do not exhibit considerable binding affinity either for central benzodiazepine or for adenosine A1-receptors.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Ansiolíticos
/
Benzodiazepinas
/
Receptores Purinérgicos P1
Límite:
Animals
Idioma:
En
Revista:
Farmaco
Asunto de la revista:
FARMACOLOGIA
/
QUIMICA
Año:
2001
Tipo del documento:
Article
País de afiliación:
Italia
Pais de publicación:
Francia