Biomedical Engineering Reference
In-Depth Information
FIGURE 17.8
Summary of Novartis HTS screening campaign.
12,000 compounds in less than a week, a job that previously would have taken months
to complete [45]. This led to the identification of 275 compounds with submicromolar
activity (Figure 17.8). Primary hits that showed toxicity or which had unfavorable
pharmacokinetic and physical properties were eliminated, and the spiroazepineindole
19 was selected as a starting point for further development.
This lead compound was prepared using Pictet-Spengler cyclization [46] and
follows a build/couple/pair strategy for developing complex diverse libraries. Thus,
synthesis of spiroazepineindole 19 involved an initial build phase (Figure 17.9) in
FIGURE 17.9
Preparation of spiroazepineindole 19 using a build/couple/pair strategy.
 
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