| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10592870 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
The chiral isomers of the two potent simplified RTX-based vanilloids, compounds 2 and 3, were synthesized employing highly enantioselective PTC alkylation and evaluated as hTRPV1 ligands. The analysis indicated that the R-isomer was the eutomer in binding affinity and functional activity. The agonism of compound 2R was comparable to that of RTX. Docking analysis of the chiral isomers of 3 suggested the basis for its stereospecific activity and the binding mode of 3R.
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Authors
Myeong Seop Kim, Yooran Ki, Song Yeon Ahn, Suyoung Yoon, Sung-Eun Kim, Hyeung-Geun Park, Wei Sun, Karam Son, Minghua Cui, Sun Choi, Larry V. Pearce, Timothy E. Esch, Ian A. DeAndrea-Lazarus, Peter M. Blumberg, Jeewoo Lee,