Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands

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 agonis...

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Publicado no:Bioorg Med Chem Lett
Main Authors: Kim, Myeong Seop, Ki, Yooran, Ahn, Song Yeon, Yoon, Suyoung, Kim, Sung-Eun, Park, Hyeung-Geun, Sun, Wei, Son, Karam, Cui, Minghua, Choi, Sun, Pearce, Larry V., Esch, Timothy E., DeAndrea-Lazarus, Ian A., Blumberg, Peter M., Lee, Jeewoo
Formato: Artigo
Idioma:Inglês
Publicado em: 2013
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6957263/
https://ncbi.nlm.nih.gov/pubmed/24321344
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2013.10.064
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