Two-colour screening in combinatorial chemistry: prospecting for enantioselectivity in a library of steroid-based receptors
Two-colour screening in combinatorial chemistry: prospecting for enantioselectivity in a library of steroid-based receptors
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DOI：
10.1016/j.tet.2009.06.018
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发表时间：
2009-08-08
期刊：
影响因子：
2.1
通讯作者：
Davis, Anthony P.
中科院分区：
文献类型：
--
作者：
del Amo, Vicente;McGlone, Adam P.;Davis, Anthony P.
用染料标记的底物对筛选树脂结合的组合文库是发现选择性受体的有力策略。然而，由于缺乏互补但化学性质相似的染料，实施受到阻碍。我们现在表明，完善的分散红1和最近推出的布里斯托蓝1可用于平行合成的“假对映体”类似物的N-乙酰基-α-氨基酸和抗炎药物Naobenzen。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，一些成员可能是N-乙酰基-α-氨基酸的高度对映选择性受体。(C)2009爱思唯尔有限公司版权所有。
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. (C) 2009 Elsevier Ltd. All rights reserved.