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Synthesis of 2-substituted-pyrrolidinethiourea derivatives and their antagonist effect on vanilloid receptor
- Authors
- Park, HG; Park, MK; Choi, JY; Choi, SH; Lee, J; Suh, YG; Oh, U; Lee, J; Kim, HD; Park, YH; Jeong, YS; Choi, JK; Jew, SS
- Issue Date
- Jan-2003
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.13, no.2, pp 197 - 200
- Pages
- 4
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 13
- Number
- 2
- Start Page
- 197
- End Page
- 200
- ISSN
- 0960-894X
1464-3405
- Abstract
- Four pyrrolidine derivatives were prepared by the formation of a 5-membered ring based on capsazepine. Among them, the two carbon extended derivatives, 4a (IC50 = 55 muM) and 4b (IC50 = 3 muM), both showed different levels of antagonist activity against the vanilloid receptor in a Ca-45(2+)-influx assay. (C) 2002 Elsevier Science Ltd. All rights reserved.
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