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

被引:74
作者
Marder, M
Viola, H
Bacigaluppo, JA
Colombo, MI
Wasowski, C
Wolfman, C
Medina, JH
Rúveda, EA
Paladini, AC
机构
[1] Univ Buenos Aires, Fac Farm & Bioquim, Inst Quim & Fisicoquim Biol, RA-1113 Buenos Aires, DF, Argentina
[2] Univ Buenos Aires, Fac Med, Inst Biol Celular & Neurociencias, RA-1121 Buenos Aires, DF, Argentina
[3] Univ Nacl Rosario, Inst Quim Organ & Sintesis, RA-2000 Rosario, Santa Fe, Argentina
关键词
D O I
10.1006/bbrc.1998.9146
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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'-fluoro-flavone; 6,3'-dichloroflavone; 6-bromo-3'-chloroflavone and 6-chloro-5'-bromoflavone. (C) 1998 Academic Press.
引用
收藏
页码:481 / 485
页数:5
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