| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369310 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ho Shin Kim, Mi-Kyoung Jin, Sang-Uk Kang, Ju-Ok Lim, Phuong-Thao Tran, Van-Hai Hoang, Jihyae Ann, Tae-Hwan Ha, Larry V. Pearce, Vladimir A. Pavlyukovets, Peter M. Blumberg, Jeewoo Lee,