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.
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea. jeewoo@snu.ac.kr
Jeewoo
J
Lee
Mi-Kyoung
MK
Jin
Sang-Uk
SU
Kang
Su Yeon
SY
Kim
Jiyoun
J
Lee
Myoungyoup
M
Shin
Jaemin
J
Hwang
Sookhyun
S
Cho
Yeon-Sil
YS
Choi
Hyun-Kyung
HK
Choi
Sung-Eun
SE
Kim
Young-Ger
YG
Suh
Yong-Sil
YS
Lee
Young-Ho
YH
Kim
Hee-Jin
HJ
Ha
Attila
A
Toth
Larry V
LV
Pearce
Richard
R
Tran
Tamas
T
Szabo
Jacqueline D
JD
Welter
Daniel J
DJ
Lundberg
Yun
Y
Wang
Jozsef
J
Lazar
Vladimir A
VA
Pavlyukovets
Matthew A
MA
Morgan
Peter M
PM
Blumberg
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