401573-22-6

Upstream product

• 421-83-0 trifluoromethane sulfonyl chloride 
• 94838-55-8 tert-butyl (4-aminobenzyl)carbamate 
• 4403-71-8 (4-aminomethyl)aniline 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 401573-32-8 N-[4-(aminomethyl)phenyl]-1,1,1-trifluoromethanesulfonamide 

Relevant academic research and scientific papers

N-4-Substituted-benzyl-N′-tert-butylbenzyl thioureas as vanilloid receptor ligands: Investigation on the role of methanesulfonamido group in antagonistic activity

A series of N-4-substituted-benzyl-N′-tert-butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG neurons. Their structure-activity relationship reveals that not only the two oxyge

N-(3-acyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues: Novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor

Isosteric replacement of the phenolic hydroxyl group in potent vanilloid receptor (VR1) agonists with the alkylsulfonamido group provides a series of compounds which are effective antagonists to the action of the capsaicin on rat VR1 heterologously expressed in Chinese hamster ovary (CHO) cells. In particular, compound 61, N-[2-(3,4-dimethylbenzyl)-3-pivaloyloxypropyl]-N′-[3-fluoro-4- (methylsulfonylamino)benzyl]thiourea was a full antagonist against capsaicin, displayed a Ki value of 7.8 nM (compared to 520 nM for capsazepine and 4 nM for 5-iodoRTX), and showed excellent analgesic activity in mice. Structure-activity analysis of the influence of modifications in the A- and C-regions of 4-methylsulfonamide ligands on VR1 agonism/antagonism indicated that 3-fluoro substitution in the A-region and a 4-tert-butylbenzyl moiety in the C-region favored antagonism, whereas a 3-methoxy group in the A-region and 3-acyloxy2-benzylpropyl moieties in the C-region favored agonism.