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Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists
- Authors
- Ryu, CH; Jang, MJ; Jung, JW; Park, JH; Choi, HY; Suh, YG; Oh, U; Park, HG; Lee, J; Koh, HJ; Mo, JH; Joo, YH; Park, YH; Kim, HD
- Issue Date
- Apr-2004
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.14, no.7, pp 1751 - 1755
- Pages
- 5
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 14
- Number
- 7
- Start Page
- 1751
- End Page
- 1755
- ISSN
- 0960-894X
1464-3405
- Abstract
- 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 muM which is 10-fold more potent than capsazepine. (C) 2004 Elsevier Ltd. All rights reserved.
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