N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.

作者信息

Park Hyeung-geun, Choi Ji-yeon, Choi Sea-hoon, Park Mi-kyung, Lee Jihye, Suh Young-ger, Cho Hawon, Oh Uhtaek, Lee Jiyoun, Kang Sang-Uk, Lee Jeewoo, Kim Hee-Doo, Park Young-Ho, Su Jeong Yeon, Kyu Choi Jin, Jew Sang-sup

机构信息

Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University, Seoul 151-742, South Korea.

出版信息

Bioorg Med Chem Lett. 2004 Feb 9;14(3):787-91. doi: 10.1016/j.bmcl.2003.11.019.

DOI:10.1016/j.bmcl.2003.11.019

PMID:14741290

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.

摘要