N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands |
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Authors: | Park Hyeung-Geun Choi Ji-Yeon Choi Sea-Hoon Park Mi-Kyung Lee Jihye Suh Young-Ger Cho Hawon Oh Uhtaek Kim Hee-Doo Joo Yung Hyup Kim Sun-Young Park Young-Ho Jeong Yeon Su Choi Jin Kyu Kim Jin Kwan Jew Sang-Sup |
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Affiliation: | Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University, Seoul 151-742, South Korea. hgpk@plaza.snu.ac.kr |
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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). |
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