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ACS Comb Sci. 2018 May 14;20(5):251-255. doi: 10.1021/acscombsci.8b00009. Epub 2018 Apr 25.

Development and Synthesis of DNA-Encoded Benzimidazole Library.

Author information

1
GlaxoSmithKline , Platform Technology & Science , 200 Cambridgepark Drive , Cambridge , Massachusetts 02140 , United States.

Abstract

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.

KEYWORDS:

DNA-encoded library technology; benzimidazole

PMID:
29648439
DOI:
10.1021/acscombsci.8b00009

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