Abstract:A novel class of potent NaV1.7 inhibitors
has been discovered.
The replacement of diaryl ether in compound I was investigated
to enhance mouse NaV1.7 inhibitory activity, which resulted
in the discovery of N-aryl indoles. The introduction
of the 3-methyl group is crucial for high NaV1.7 in vitro
potency. The adjustment of lipophilicity led to the discovery of 2e. Compound 2e (DS43260857) demonstrated high
in vitro potencies against both human and mouse NaV1.7
with high selectivity over NaV1.1, NaV1.5, and
hERG… Show more
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