Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.
The structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. The 2-halogen analogues showed enhanced antagonism compared to the prototype antagonist.
Lee
Jeewoo
J
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea. jeewoo@snu.ac.kr
Kang
Sang-Uk
SU
Kil
Min-Jung
MJ
Shin
Myoungyoup
M
Lim
Ju-Ok
JO
Choi
Hyun-Kyung
HK
Jin
Mi-Kyoung
MK
Kim
Su Yeon
SY
Kim
Sung-Eun
SE
Lee
Yong-Sil
YS
Min
Kyung-Hoon
KH
Kim
Young-Ho
YH
Ha
Hee-Jin
HJ
Tran
Richard
R
Welter
Jacqueline D
JD
Wang
Yun
Y
Szabo
Tamas
T
Pearce
Larry V
LV
Lundberg
Daniel J
DJ
Toth
Attila
A
Pavlyukovets
Vladimir A
VA
Morgan
Matthew A
MA
Blumberg
Peter M
PM
D000818:Animals; D016466:CHO Cells; D002118:Calcium / Q000378:metabolism; D006224:Cricetinae; D008024:Ligands; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013890:Thiourea / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*
D008024:Ligands; C505274:N-(4-t-butylbenzyl)-N'-(4-(methylsulfonylamino)benzyl)thiourea; D013449:Sulfonamides; D050916:TRPV Cation Channels; C494484:TRPV1 receptor; D013890:Thiourea; D002118:Calcium