910534-78-0

Upstream product

• 1208-65-7 4-tert-butyl-trans-cinnamic acid 
• 694529-76-5 (S)-4-methanesulfonamido-α-methylbenzylamine 
• 910534-77-9 (R)-3-(4-t-butylphenyl)-N-[1-(4-methanesulfonylaminophenyl)ethyl]acrylamide 

Relevant academic research and scientific papers

2-Methylacrylamide as a bioisoster of thiourea group for 1,3-dibenzylthioureido TRPV1 receptor antagonists

In order to replace thiourea group with the more drug-like moiety for 1,3-dibenzylthioureas having TRPV1 antagonist activity, we introduced a set of functional groups between the two aromatic rings based on bioisosteric replacement. The synthesized bioisosteres of 1,3-dibenzylthioureas were tested for their antagonist activities on TRPV1 by 45Ca2+-influx assay using neonatal rat cultured spinal sensory neurons. Among the tested 14 kinds of bioisosters, 2-methylacrylamide group was the best candidate to replace thiourea group. Compound 7c, 2-methylacrylamide analog of ATC-120, showed as potent as ATC-120 in its antagonist activity. In addition, 2-methylacrylamide analog 7e having vinyl moiety showed the most potent activity with 0.022 μM of IC50 value, indicating that thiourea group of 1,3-dibenzylthioureas could be replaced to 2-methylacrylamide without loss of their potencies.

NOVEL COMPOUNDS, ISOMER THEREOF OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1 )antagonist; and a pharmaceutical composition containing the same. The present invention