Encoded library technology (ELT) is an effective approach to the discovery of novel small-molecule ligands for biological targets. A key factor for the success of the technology is the chemical diversity of the libraries. Here we report the development of DNA-conjugated benzimidazoles. Using 4-fluoro-3-nitrobenzoic acid as a key synthon, we synthesized a 320 million-member DNA-encoded benzimidazole library using Fmoc-protected amino acids, amines and aldehydes as diversity elements. Affinity selection of the library led to the discovery of a novel, potent and specific antagonist of the NK3 receptor.

中文翻译：

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DNA编码苯并咪唑文库的开发与合成

编码文库技术（ELT）是发现用于生物靶标的新型小分子配体的有效方法。技术成功的关键因素是文库的化学多样性。在这里，我们报告了DNA共轭苯并咪唑的发展。使用4-氟-3-硝基苯甲酸作为关键的合成子，我们使用Fmoc保护的氨基酸，胺和醛作为多样性元素，合成了3.2亿个DNA编码的苯并咪唑文库。文库的亲和力选择导致了新型，有效和特异性的NK3受体拮抗剂的发现。