Detection of benzodiazepine receptor ligands in small libraries of flavone derivatives synthesized by solution phase combinatorial chemistry.
Solution phase combinatorial synthesis of flavone derivatives and evaluation of their affinity for the central benzodiazepine receptors is described. The libraries preparation is simple and provides a convenient method for rapid compound generation and screening. Thirty one new compounds were obtained of which the most promising, as high affinity benzodiazepine receptor ligands, were 6-bromo-3'-fluoroflavone; 6,3'-dichloroflavone; 6-bromo-3'-chloroflavone and 6-chloro-3'-bromoflavone.
Marder
M
M
Facultad de Farmacia y Bioquímica, Instituto de Química y Fisicoquímica Biológicas, Junín 956, Buenos Aires, 1113, Argentina.
Viola
H
H
Bacigaluppo
J A
JA
Colombo
M I
MI
Wasowski
C
C
Wolfman
C
C
Medina
J H
JH
Rúveda
E A
EA
Paladini
A C
AC
D000818:Animals; D001667:Binding, Competitive; D002462:Cell Membrane / Q000378:metabolism; D002531:Cerebellum / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D005419:Flavonoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D005445:Flunitrazepam / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*; D012996:Solutions; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
D005419:Flavonoids; D011963:Receptors, GABA-A; D012996:Solutions; D005680:gamma-Aminobutyric Acid; D005445:Flunitrazepam