Synthesis and benzodiazepine receptors affinity of 2,3-dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinolin-1-one and 3-carbethoxy-4-phenylquinoline derivatives.
A series of 2,3-dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinolin-1-one derivatives and related compounds were tested for their ability to bind benzodiazepine receptors (BZRs). Most of the synthesized compounds showed micromolar affinity for BZR peripheral type, but not for the central one, with the exception of compound 4m which displayed an IC50 = 0.407 microM, only 2 fold higher than IC50 for chlordiazepoxide.
Anzini
M
M
Dipartimento Farmaco Chimico Tecnologico, Università Banchi di Sotto, Siena, Italy.
Cappelli
A
A
Vomero
S
S
Cagnotto
A
A
Skorupska
M
M
D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects; D066298:In Vitro Techniques; D051379:Mice; D008815:Mice, Inbred Strains; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects*
D011758:Pyrroles; D015363:Quinolones; D011963:Receptors, GABA-A