Chemistry Reference
In-Depth Information
The compounds prepared (Fig.
6
) and tested proved to be potent EP
1
receptor
antagonists. For the compound where R was i-Bu, the result presented was
binding pIC
50
of 8.2 and a pKi of 9.3±0.3 in a functional assay. The SAR also
showed that large groups (CH
2
CH
2
t
-Bu) are the best choice.
Figure 6:
SAR for the EP
1
receptor antagonists proposed by Hall
et al
. [33].
BIOISOSTERIC REPLACEMENTS AS A STRATEGY TO IMPROVE
SYNTHETIC ACCESSIBILITY
Chemical synthesis is an important issue and often a limiting factor in the drug
discovery process [34]. Although bioinformatics, chemoinformatics and
