Published in
Elsevier, Bioorganic and Medicinal Chemistry Letters, 12(24), p. 2685-2688, 2014
DOI: 10.1016/j.bmcl.2014.04.054
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α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists
,
Jihyae Ann,
Tae-Hwan Ha,
Larry V. Pearce,
Vladimir A. Pavlyukovets,
Peter M. Blumberg,
Jeewoo Lee
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Abstract
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.