1003002-86-5Relevant academic research and scientific papers
α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists
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
, p. 2685 - 2688 (2015/02/19)
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.
Stereospecific high-affinity TRPV1 antagonists: Chiral N-(2-benzyl-3- pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues
Ryu, Hyungchul,Jin, Mi-Kyoung,Su, Yeon Kim,Choi, Hyun-Kyung,Kang, Sang-Uk,Dong, Wook Kang,Lee, Jeewoo,Pearce, Larry V.,Pavlyukovets, Vladimir A.,Morgan, Matthew A.,Tran, Richard,Toth, Attila,Lundberg, Daniel J.,Blumberg, Peter M.
, p. 57 - 67 (2008/09/18)
Previously, we reported the thiourea antagonists 2a and 2b as potent and high affinity TRPV1 antagonists. For further optimization of the lead compounds, a series of their amide and α-substituted amide surrogates were investigated and novel chiral N-(2-be
