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Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists
- Authors
- Li, Fu-Nan; Kim, Nam-Jung; Paek, Seung-Mann; Kwon, Do-Yeon; Min, Kyung Hoon; Jeong, Yeon-Su; Kim, Sun-Young; Park, Young-Ho; Kim, Hee-Doo; Park, Hyeung-Geun; Suh, Young-Ger
- Issue Date
- May-2009
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Diarylalkyl amides; TRPV1 antagonists
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.17, no.10, pp 3557 - 3567
- Pages
- 11
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 17
- Number
- 10
- Start Page
- 3557
- End Page
- 3567
- ISSN
- 0968-0896
1464-3391
- Abstract
- We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent Ca-45(2+) uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC50 of 57 nM. The synthesis and structure-activity relationship of the diarylalkyl amides are also described. (C) 2009 Elsevier Ltd. All rights reserved.
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