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 Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Kim HS,Jin MK,Kang SU,Lim JO,Tran PT,Hoang VH,Ann J,Ha TH,Pearce LV,Pavlyukovets VA,Blumberg PM,Lee Jdoi
10.1016/j.bmcl.2014.04.054subject
Has Abstractpub_date
2014-06-15 00:00:00pages
2685-8issue
12eissn
0960-894Xissn
1464-3405pii
S0960-894X(14)00402-8journal_volume
24pub_type
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