Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists

Abstract

We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent 45Ca 2+ uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC 50 of 57 nM. The synthesis and structure–activity relationship of the diarylalkyl amides are also described.