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

Article abstract of DOI:10.1016/j.bmc.2009.04.010

We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent ⁴⁵Ca²⁺ uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC₅₀ of 57 nM. The synthesis and structure-activity relationship of the diarylalkyl amides are also described.