N-(3-Acyloxy-2-benzylpropyl)-N′-(4-hydroxy-3-methoxybenzyl) thiourea derivatives as potent vanilloid receptor agonists and analgesics

…, YH Park, VE Marquez, M Beheshti, T Szabo…

Index: Lee, Jeewoo; Lee, Jiyoun; Kim, Jiyoung; Kim, Soo Yeon; Chun, Moon Woo; Cho, Hawon; Hwang, Sun Wook; Oh, Uhtaek; Park, Young Ho; Marquez, Victor E.; Beheshti, Maryam; Szabo, Tamas; Blumberg, Peter M. Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 1 p. 19 - 32

Full Text: HTML

Citation Number: 57

Abstract

A series of N-(3-acyloxy-2-benzylpropyl)-N′-(4-hydroxy-3-methoxybenzyl) thiourea derivatives were investigated as vanilloid receptor ligands in an effort to discover a novel class of analgesics. The proposed pharmacophore model of resiniferatoxin, which includes the C20-homovanillic moiety, the C3-carbonyl and the orthoester phenyl ring as key pharmacophoric groups, was utilized as a guide for drug design. The compounds were ...