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

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.

journal_name

Bioorg Med Chem Lett

authors

Kim HS,Jin MK,Kang SU,Lim JO,Tran PT,Hoang VH,Ann J,Ha TH,Pearce LV,Pavlyukovets VA,Blumberg PM,Lee J

doi

10.1016/j.bmcl.2014.04.054

subject

Has Abstract

pub_date

2014-06-15 00:00:00

pages

2685-8

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00402-8

journal_volume

24

pub_type

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