期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 10, 页码 3557-3567出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.04.010
关键词
Diarylalkyl amides; TRPV1 antagonists
资金
- AmorePacific Corporation
- Korea Science and Engineering Foundation [R01-2007-000-20052-0]
- National Research Foundation of Korea [R01-2007-000-20052-0] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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