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Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template
- Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template
- Ann, Jihyae; Sun, Wei; Zhou, Xing; Jung, Aeran; Baek, Jisoo; Lee, Sunho; Kim, Changhoon; Yoon, Suyoung; Hong, Sunhye; Choi, Sun; Turcios, Noe A.; Herold, Brienna K. A.; Esch, Timothy E.; Lewin, Nancy E.; Abramovitz, Adelle; Pearce, Larry V.; Blumberg, Peter M.; Lee, Jeewoo
- Ewha Authors
- SCOPUS Author ID
- Issue Date
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- 0960-894X; 1464-3405
- vol. 26, no. 15, pp. 3603 - 3607
- Vanilloid receptor 1; TRPV1 antagonists; Analgesic
- PERGAMON-ELSEVIER SCIENCE LTD
- SCI; SCIE; SCOPUS
- A series of homologous analogues of prototype antagonist 1 and its urea surrogate were investigated as hTRPV1 ligands. Through one-carbon elongation in the respective pharmacophoric regions, N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea was identified as a novel and potent TRPV1 antagonistic template. Its representative compound 27 showed a potency comparable to that of lead compound 1. Docking analysis of compound 27 in our hTRPV1 homology model indicated that its binding mode was similar with that of 1S. (C) 2016 Elsevier Ltd. All rights reserved.
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