Combination of click chemistry and sulfonamides to develop three-armed triazole compounds through Biotage Isolera耐士科技

2015/02/13   下载量： 1 次

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Fragment-based drug discovery is a valuable tool in hit identification, as well as the combination of different small fragments showing a minimal binding activity against biological receptors or enzymes to give merged hits. A high number of fragments on the same scaffold improve the probability to find a candidate showing single- or multi-target affinities. A rapid and versatile approach for synthesizing libraries of densely fragment-functionalized scaffolds is reported. Many fragments were assembled in few steps around a triazole ring starting from amino alcohols and other readily available building blocks. A binding assay against integrin avb3 was used as a test-bed in order to demonstrate the potential of such an approach in hit discovery strategies.

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