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

作者：Kim Ho Shin; Jin Mi Kyoung; Kang Sang Uk; Lim Ju Ok; Phuong Thao Tran; Van Hai Hoang; Ann Jihyae; Ha Tae Hwan; Pearce Larry V; Pavlyukovets Vladimir A; Blumberg Peter M; Lee Jeewoo^*

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(12): 2685-2688.

DOI：10.1016/j.bmcl.2014.04.054

• Vanilloid receptor 1
• TRPV1 antagonist
• Capsaicin
• Resiniferatoxin

A series of alpha-methylated analogues of the potent sRTX thiourea antagonists were investigated as rTRPV1 ligands in order to examine the effect of alpha-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.

• 出版日期2014-6-15