In the July 2018 issue of SLAS Discovery, a review article summarizes new methods of fragment-based lead discovery (FBLD) to identify new compounds as potential antibiotics.
Authors Bas Lamoree and Roderick E. Hubbard of the University of York (UK) explain how FBLD works and illustrate its advantages over conventional high-throughput screening (HTS). Specifically, how FBLD increases the chances of finding hit compounds; how its methods can deliver hits without the massive investment required for HTS; and how by starting small, FBLD gives medicinal chemists more opportunities to build more drug-like compounds. These principles are illustrated in the review and supported with recent examples of discovery projects against a range of potential...