title: N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.
abstract: A series of N-4-substituted-benzyl-N'-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 not only the two oxygens and amide hydrogen of sulfonamido group, but also the optimal size of methyl in methanesulfonamido group play an integral role for the antagonistic activity on vanilloid receptor.
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: Jiyoun
authors.initials: J
authors.lastname: Lee
authors.forename: Sang-Uk
authors.initials: SU
authors.lastname: Kang
authors.forename: Jeewoo
authors.initials: J
authors.lastname: Lee
authors.forename: Hee-Doo
authors.initials: HD
authors.lastname: Kim
authors.forename: Young-Ho
authors.initials: YH
authors.lastname: Park
authors.forename: Yeon
authors.initials: Y
authors.lastname: Su Jeong
authors.forename: Jin
authors.initials: J
authors.lastname: Kyu Choi
authors.forename: Sang-sup
authors.initials: SS
authors.lastname: Jew
mesh_terms: D000818:Animals; D000831:Animals, Newborn; D002118:Calcium / Q000378:metabolism; D002211:Capsaicin / Q000378:metabolism*; D002478:Cells, Cultured; D005727:Ganglia, Spinal / Q000187:drug effects; D008024:Ligands; D015394:Molecular Structure; D009474:Neurons / Q000187:drug effects*; D051381:Rats; D011955:Receptors, Drug / Q000819:agonists / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology*; D013890:Thiourea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D008024:Ligands; D011955:Receptors, Drug; D013449:Sulfonamides; D013890:Thiourea; D002211:Capsaicin; D002118:Calcium