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Bioorg Med Chem Lett. 2014 Jun 15;24(12):2685-8. doi: 10.1016/j.bmcl.2014.04.054. Epub 2014 Apr 23.

α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists.

Author information

  • 1Laboratory of Medicinal Chemistry, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
  • 2Laboratory of Cancer Biology and Genetics, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.
  • 3Laboratory of Medicinal Chemistry, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea. Electronic address: jeewoo@snu.ac.kr.

Abstract

A series of α-methylated analogues of the potent sRTX thiourea antagonists were investigated as rTRPV1 ligands in order to examine the effect of α-methylation on receptor activity. The SAR analysis indicated that activity was stereospecific with the (R)-configuration of the newly formed chiral center providing high binding affinity and potent antagonism while the configuration of the C-region was not significant.

Copyright © 2014 Elsevier Ltd. All rights reserved.

KEYWORDS:

Capsaicin; Resiniferatoxin; TRPV1 antagonist; Vanilloid receptor 1

PMID:
24794110
[PubMed - indexed for MEDLINE]
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