Detection of benzodiazepine receptors ligands in small libraries of flavone derivatives synthesized by solution phase combinatorial chemistry.

M. MARDER; H. VIOLA; J. A. BACIGALUPPO; M. I. COLOMBO; C. WASOWSKI; C. WOLFMAN; J. H. MEDINA; E. A. RUVEDA; A. C. PALADINI

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Año: 1998 vol. 249 p. 481 - 485

0006-291X

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 screening. Thirty one new compounds were obtained of which the most promising, as high affinity benzodiazepine receptor ligands, were 6-bromo-3´-fluoro- flavone; 6,3´-dichloroflavone; 6-bromo-3´-chloroflavone and 6-chloro-3´-bromoflavone.derivatives and evaluation of their affinity for the central benzodiazepine receptors is described. The libraries preparation is simple and provides a convenient method screening. Thirty one new compounds were obtained of which the most promising, as high affinity benzodiazepine receptor ligands, were 6-bromo-3´-fluoro- flavone; 6,3´-dichloroflavone; 6-bromo-3´-chloroflavone and 6-chloro-3´-bromoflavone.