N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.
A series of N-4-methansulfonamidobenzyl-N'-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 (IC(50)=15 nM).
Park
Hyeung-Geun
HG
Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University, Seoul 151-742, South Korea. hgpk@plaza.snu.ac.kr
Choi
Ji-Yeon
JY
Choi
Sea-Hoon
SH
Park
Mi-Kyung
MK
Lee
Jihye
J
Suh
Young-Ger
YG
Cho
Hawon
H
Oh
Uhtaek
U
Kim
Hee-Doo
HD
Joo
Yung Hyup
YH
Kim
Sun-Young
SY
Park
Young-Ho
YH
Jeong
Yeon Su
YS
Choi
Jin Kyu
JK
Kim
Jin Kwan
JK
Jew
Sang-Sup
SS
D000818:Animals; D002478:Cells, Cultured; D005727:Ganglia, Spinal / Q000187:drug effects / Q000378:metabolism; D008024:Ligands; D051381:Rats; D011955:Receptors, Drug / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013449:Sulfonamides / Q000737:chemistry* / Q000378:metabolism; D013890:Thiourea / Q000737:chemistry* / Q000378:metabolism
D008024:Ligands; D011955:Receptors, Drug; D013449:Sulfonamides; D013890:Thiourea