N-4-Methansulfonamidobenzyl-N′-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands

H Park, J Choi, S Choi, M Park, J Lee, YG Suh…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 7 p. 1693 - 1696

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Citation Number: 13

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 ...