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α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Jun 15; Vol. 24 (12), pp. 2685-8. Date of Electronic Publication: 2014 Apr 23. - Publication Year :
- 2014
-
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.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
CHO Cells
Cricetinae
Cricetulus
Diterpenes chemistry
Humans
Methylation
Molecular Structure
Protein Binding drug effects
Rats
Stereoisomerism
Structure-Activity Relationship
Thiourea analogs & derivatives
Thiourea chemistry
Diterpenes chemical synthesis
Diterpenes pharmacology
TRPV Cation Channels antagonists & inhibitors
Thiourea chemical synthesis
Thiourea pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 24
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24794110
- Full Text :
- https://doi.org/10.1016/j.bmcl.2014.04.054