EaStCHEM School of Chemistry, University of Edinburgh, Joseph Black Building, David Brewster Road, Edinburgh, EH9 3FJ, UK.
Org Biomol Chem. 2018 Nov 7;16(43):8144-8149. doi: 10.1039/c8ob01918e.
Dynamic combinatorial chemistry (DCC) is a powerful tool to identify ligands for biological targets. We used 19F NMR as an in situ, non-invasive technique for measuring the composition of a dynamic combinatorial library (DCL) of N-acylhydrazones (NAHs). An NAH DCL, constructed from a fluoro-aromatic aldehyde and a small set of hydrazides, was targetted at ecFabH, an essential enzyme in bacterial fatty acid biosynthesis. Our NMR analysis identified a tert-butyl NAH as the best binder which was confirmed by enzymatic assay.
动态组合化学（DCC）是一种鉴定生物靶标配体的强大工具。我们使用 19F NMR 作为一种原位、非侵入性技术来测量 N-酰腙（NAH）的动态组合文库（DCL）的组成。NAH DCL 由氟芳基醛和一小部分酰肼构建而成，针对的是细菌脂肪酸生物合成中的必需酶 ecFabH。我们的 NMR 分析确定叔丁基 NAH 是最好的结合物，这一点通过酶测定得到了证实。
