Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
The structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. A docking model of potent antagonist 2 with the sensor region of TRPV1 is proposed.
Lee
Jeewoo
J
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea. jeewoo@snu.ac.kr
Jin
Mi-Kyoung
MK
Kang
Sang-Uk
SU
Kim
Su Yeon
SY
Lee
Jiyoun
J
Shin
Myoungyoup
M
Hwang
Jaemin
J
Cho
Sookhyun
S
Choi
Yeon-Sil
YS
Choi
Hyun-Kyung
HK
Kim
Sung-Eun
SE
Suh
Young-Ger
YG
Lee
Yong-Sil
YS
Kim
Young-Ho
YH
Ha
Hee-Jin
HJ
Toth
Attila
A
Pearce
Larry V
LV
Tran
Richard
R
Szabo
Tamas
T
Welter
Jacqueline D
JD
Lundberg
Daniel J
DJ
Wang
Yun
Y
Lazar
Jozsef
J
Pavlyukovets
Vladimir A
VA
Morgan
Matthew A
MA
Blumberg
Peter M
PM
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D008024:Ligands; D008958:Models, Molecular; D017434:Protein Structure, Tertiary; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D013859:Thiocarbamates / Q000138:chemical synthesis / Q000737:chemistry; 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; D013859:Thiocarbamates; D013890:Thiourea