911124-97-5

Upstream product

• 152918-49-5 O-tert-butyl-4-amino-3-iodobenzylcarbamate 
• 124-63-0 methanesulfonyl chloride 
• 873-74-5 4-Aminobenzonitrile 
• 33348-34-4 4-amino-3-iodobenzonitrile 
• 106941-22-4 4-amino-3-iodobenzylamine 

Downstream Products

• 1196702-90-5 C₁₄H₁₉N₃O₄S 
• 911124-02-2 tert-butyl 4-(methylsulfonamido)-3-vinylbenzylcarbamate 

Relevant academic research and scientific papers

Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists

Structural optimization of multiple H-bonding region and structure-activity relationship of diarylalkyl amides/thioamides as novel TRPV1 antagonists are described. In particular, we identified amide 34o and thioamides 35o and 35r, of which antagonistic activities were highly enhanced by an incorporation of cyano or vinyl-substituent to the multiple H-bonding region. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron with IC50s of 25, 32 and 28 nM, respectively.

Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: Structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents

Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure-activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure-activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit Ca2+ uptake inhibition in rat DRG neuron with IC50 between 10 and 100 nM.