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

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 cente...

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Publicat a:Bioorg Med Chem Lett
Autors principals: Kim, Ho Shin, Jin, Mi-Kyoung, Kang, Sang-Uk, Lim, Ju-Ok, Tran, Phuong-Thao, Hoang, Van-Hai, Ann, Jihyae, Ha, Tae-Hwan, Pearce, Larry V., Pavlyukovets, Vladimir A., Blumberg, Peter M., Lee, Jeewoo
Format: Artigo
Idioma:Inglês
Publicat: 2014
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC6957243/
https://ncbi.nlm.nih.gov/pubmed/24794110
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2014.04.054
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