Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Design, synthesis and biological evaluation of B-region modified diarylalkyl amide analogues as novel TRPV1 antagonists.

Authors: Young Taek Han, Shao-Mei Yang, Xiao-Yuan Wang, Fu-Nan Li

Journal, date & volume: Arch. Pharm. Res., 2014 Apr , 37, 440-51

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23943439

Abstract
Design, synthesis and biological evaluation of B-region, known to be a dipolar interacting pharmacophore, modified diarylalkyl amide analogues for novel TRPV1 (transient receptor potential channel, vanilloid subfamily member 1) antagonists was described. A variety of moieties including guanidines, heterocyclic rings, cinnamides, and α-substituted acetamides were introduced at the B-region. TRPV1 antagonistic activities of these analogues were evaluated by (45)Ca(2+) uptake assay in rat DRG neuron. In particular, α,α-difluoroamide 53 exhibited 3-fold more potent TRPV1 antagonistic activity (IC50 = 0.058 μM) than the parent amide analogue 6.