Structure-activity relationships of 2-aryl-2,5-dihydropyridazino [4,3-b]indol-3(3H)-ones at the benzodiazepine receptor.
Bioorg Med Chem
; 4(12): 2091-104, 1996 Dec.
Article
en En
| MEDLINE
| ID: mdl-9022974
ABSTRACT
A large series of 2-aryl-2,5-dihydropyridazino[4,3-b]indol-3(3H)ones (PIs) carrying properly selected substituents at the indole and N2-phenyl rings was prepared and tested as central benzodiazepine receptor (BZR) ligands and potential (anti)convulsant agents. Stereoelectronic requirements for high receptor affinity were detected by means of 2-D and 3-D QSAR analyses. BZR affinities and pharmacological profiles of the compounds were examined in comparison with some other pyridazinoindolones recently described by us and with pyrazoloquinoline (PQ) analogues. An anticonvulsant activity greater than PQs was generally observed for PIs. Notably, in the test of audiogenically induced seizures, one compound showed a potency comparable to that of diazepam.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Piridazinas
/
Receptores de GABA-A
/
Indoles
/
Anticonvulsivantes
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
1996
Tipo del documento:
Article
País de afiliación:
Italia