Biomedical Engineering Reference
In-Depth Information
FIGURE 17.2
Overview of a build/couple/pair strategy.
Due to its modular approach, DOS strategies allow systematic access to diverse
compounds. Already shown was the utilization of a build/couple/pair strategy allow-
ing access to stereochemically diverse scaffolds in an efficient manner. Incorporation
of desirable or more drug-like properties is also possible by upfront evaluation of
the building blocks utilized, either in the synthesis of the scaffold or appendage
diversification through library production.
The latter concepts was the focus of work presented by Akella and Marcaurelle
[10]. Library design focused on a logical sparse matrix design, making compounds
with appropriate building block combinations rather than a full matrix approach where
all building block combinations are synthesized. The building block combinations
