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N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands

Authors
Park, HGChoi, JYChoi, SHPark, MKLee, JSuh, YGCho, HOh, UKim, HDJoo, YHKim, SYPark, YHJeong, YSChoi, JKKim, JKJew, SS
Issue Date
Apr-2004
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
vanilloid receptor; antagonist; structure-activity relationship
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.14, no.7, pp 1693 - 1696
Pages
4
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
14
Number
7
Start Page
1693
End Page
1696
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/15889
DOI
10.1016/j.bmcl.2004.01.041
ISSN
0960-894X
1464-3405
Abstract
A series of N-4-methansulfonamidobenzyl-M-2-substituted-4-tert-butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG neurons. Their structure-activity relationship reveals that there is a space for another hydrophobic binding interaction around 2-position in 4-tert-butylbenzyl region. Among the prepared derivatives, 6n show the highest antagonistic activity against the vanilloid receptor (IC50 = 15 nM). (C) 2004 Elsevier Ltd. All rights reserved.
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