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Two-colour screening in combinatorial chemistry: prospecting for enantioselectivity in a library of steroid-based receptors

机译:组合化学中的双色筛选:在基于类固醇的受体库中对映选择性的前景

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The screening of resin-bound combinatorial libraries with pairs of dye-tagged substrates is a powerful strategy for discovering selective receptors. However, implementation has been hampered by a lack of complementary but chemically similar dyes. We now show that the well-established Disperse Red 1 and the recently-introduced Bristol Blue 1 can be used in parallel to synthesise 'pseudoenantiomeric' analogues of N-acetyl-alpha-amino acids and of the anti-inflammatory drug Naproxen. A steroid-based receptor library has been prepared and screened with these substrates. Preliminary results suggest that some members may be highly enantioselective receptors for N-acetyl-alpha-amino acids.
机译:用成对的染料标记底物对树脂结合的组合文库进行筛选是发现选择性受体的有力策略。但是,由于缺乏互补的但化学上相似的染料,实施受到了阻碍。我们现在显示,成熟的分散红1和最近引入的布里斯托尔蓝1可以并行使用,以合成N-乙酰-α-氨基酸和消炎药萘普生的“假对映异构”类似物。已经制备了基于类固醇的受体文库,并用这些底物进行了筛选。初步结果表明,某些成员可能是N-乙酰基-α-氨基酸的高度对映选择性受体。

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