1002126-15-9

Upstream product

• 1002127-15-2 ethyl (E)-5,5-dibromo-2,4-pentadienoate 
• 1125-60-6 isoquinolin-5-ylamine 
• 1176922-03-4 C₂₂H₂₀F₃NO₃ 

Relevant academic research and scientific papers

Discovery of novel 5,5-diarylpentadienamides as orally available transient receptor potential vanilloid 1 (TRPV1) antagonists

We have developed a novel and potent chemical series of 5,5-diphenylpentadienamides for targeting TRPV1 in vitro and in vivo. In this investigation, we examined a variety of replacements for the 5-position of dienamides with the goal of addressing issues related to pharmacokinetics. Our data suggest that substitution with alkoxy groups on the phenyl ring at the 5-position increases their ability to penetrate the blood-brain barrier. This investigation culminated in the discovery of compound (R)-36b, which showed a good pharmacokinetic profile. In vivo, compound (R)-36b was found to be effective at reversing mechanical allodynia in rats in a dose-dependent manner, and it reversed thermal hyperalgesia in a model of neuropathic pain induced by sciatic nerve injury.

PENTADIENAMIDE DERIVATIVE

The present invention provides a pentadienamide derivative represented by the formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents substitu