HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Discovery of piperidine carboxamide TRPV1 antagonists.

Abstract
A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential vanilloid-1 (TRPV1), an emerging target for the treatment of pain. A focused library of polar head groups led to the identification of a benzoxazinone amide that afforded good potency in cell-based assays. Synthesis and a QSAR model will be presented.
AuthorsWing S Cheung, Raul R Calvo, Brett A Tounge, Sui-Po Zhang, Dennis R Stone, Michael R Brandt, Tasha Hutchinson, Christopher M Flores, Mark R Player
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 18 Issue 16 Pg. 4569-72 (Aug 15 2008) ISSN: 1464-3405 [Electronic] England
PMID18662879 (Publication Type: Journal Article)
Chemical References
  • Amides
  • Benzoxazines
  • Carrier Proteins
  • Piperidines
  • TRPV Cation Channels
  • TRPV1 protein, human
  • Capsaicin
Topics
  • Amides (chemistry)
  • Benzoxazines (chemistry, pharmacology)
  • Capsaicin (chemistry)
  • Carrier Proteins (antagonists & inhibitors)
  • Chemistry, Pharmaceutical (methods)
  • Drug Design
  • Humans
  • Inhibitory Concentration 50
  • Models, Chemical
  • Molecular Conformation
  • Piperidines (chemistry)
  • Protein Binding
  • Quantitative Structure-Activity Relationship
  • Structure-Activity Relationship
  • TRPV Cation Channels (antagonists & inhibitors)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: