Ontology highlight
ABSTRACT:
SUBMITTER: Kitamura S
PROVIDER: S-EPMC7751259 | biostudies-literature | 2020 Jun
REPOSITORIES: biostudies-literature
Journal of the American Chemical Society 20200610 25
Optimization of small-molecule probes or drugs is a synthetically lengthy, challenging, and resource-intensive process. Lack of automation and reliance on skilled medicinal chemists is cumbersome in both academic and industrial settings. Here, we demonstrate a high-throughput hit-to-lead process based on the biocompatible sulfur(VI) fluoride exchange (SuFEx) click chemistry. A high-throughput screening hit benzyl (cyanomethyl)carbamate (<i>K</i><sub>i</sub> = 8 μM) against a bacterial cysteine p ...[more]