Chain-branched 1, 3-dibenzylthioureas as vanilloid receptor 1 antagonists

…, JH Park, HY Choi, Y Suh, U Oh, H Park, J Lee…

文献索引：Ryu, Chong Hyun; Jang, Mi Jung; Jung, Jeong Wha; Park, Ju-Hyun; Choi, Hye Young; Suh, Young-Ger; Oh, Uhtaek; Park, Hyeung-Geun; Lee, Jeewoo; Koh, Hyun-Joo; Mo, Joo-Hyun; Joo, Yung Hyup; Park, Young-Ho; Kim, Hee-Doo Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 7 p. 1751 - 1755

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被引用次数: 15

摘要

A series of chain-branched 1, 3-dibenzylthiourea derivatives were synthesized, and tested their antagonist activity against vanilloid receptor 1. Chain-branching led to a significant change in the mode of action and the potency.(R)-Methyl or ethyl-branched 1, 3- dibenzylthiourea derivatives showed the most potent antagonist activity up to the IC50 value of 0.05 μM which is 10-fold more potent than capsazepine.