Author/Authors :
Hyeung-geun Park، نويسنده , , Ji-yeon Choi، نويسنده , , Sea-hoon Choi، نويسنده , , Mi-kyung Park، نويسنده , , Jihye Lee، نويسنده , , Young-Ger Suh، نويسنده , , Hawon Cho، نويسنده , , Uhtaek Oh، نويسنده , , Hee-Doo Kim، نويسنده , , Yung Hyup Joo، نويسنده , , Sun-Young Kim، نويسنده , , Young-Ho Park، نويسنده , , Yeon Su Jeong، نويسنده , , Jin Kyu Choi، نويسنده , , Jin-Kwan Kim، نويسنده , , Sang-sup Jew، نويسنده ,
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 (IC50=15 nM).
Keywords :
e-mail: hgpk@plaza.snu.ac.kr , Vanilloid receptor , Antagonist , Structure–activity relationship.* Corresponding authors. Tel.: +82-2880-7871 , fax: +82-2872-9129
