title: N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.
abstract: 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).
authors.affiliation: Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University, Seoul 151-742, South Korea. hgpk@plaza.snu.ac.kr
authors.forename: Hyeung-Geun
authors.initials: HG
authors.lastname: Park
authors.forename: Ji-Yeon
authors.initials: JY
authors.lastname: Choi
authors.forename: Sea-Hoon
authors.initials: SH
authors.lastname: Choi
authors.forename: Mi-Kyung
authors.initials: MK
authors.lastname: Park
authors.forename: Jihye
authors.initials: J
authors.lastname: Lee
authors.forename: Young-Ger
authors.initials: YG
authors.lastname: Suh
authors.forename: Hawon
authors.initials: H
authors.lastname: Cho
authors.forename: Uhtaek
authors.initials: U
authors.lastname: Oh
authors.forename: Hee-Doo
authors.initials: HD
authors.lastname: Kim
authors.forename: Yung Hyup
authors.initials: YH
authors.lastname: Joo
authors.forename: Sun-Young
authors.initials: SY
authors.lastname: Kim
authors.forename: Young-Ho
authors.initials: YH
authors.lastname: Park
authors.forename: Yeon Su
authors.initials: YS
authors.lastname: Jeong
authors.forename: Jin Kyu
authors.initials: JK
authors.lastname: Choi
authors.forename: Jin Kwan
authors.initials: JK
authors.lastname: Kim
authors.forename: Sang-Sup
authors.initials: SS
authors.lastname: Jew
mesh_terms: 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
chemical_list: D008024:Ligands; D011955:Receptors, Drug; D013449:Sulfonamides; D013890:Thiourea