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Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: Structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents

Authors
Suh, YGLee, YSMin, KHPark, OHKim, JKSeung, HSSeo, SYLee, BYNam, YHLee, KOKim, HDPark, HGLee, JOh, ULim, JOKang, SUKil, MJKoo, JYShin, SSJoo, YHKim, JKJeong, YSKim, SYPark, YH
Issue Date
Sep-2005
Publisher
AMER CHEMICAL SOC
Citation
JOURNAL OF MEDICINAL CHEMISTRY, v.48, no.18, pp 5823 - 5836
Pages
14
Journal Title
JOURNAL OF MEDICINAL CHEMISTRY
Volume
48
Number
18
Start Page
5823
End Page
5836
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/15475
DOI
10.1021/jm0502790
ISSN
0022-2623
1520-4804
Abstract
Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure-activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure- activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit Ca2+ uptake inhibition in rat DRG neuron with IC50 between 10 and 100 nM.
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