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新型二芳基烷基酰胺作为瞬时受体电位香草酸亚型1（TRPV1）拮抗剂的设计、合成及生物学评价

Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists.

作者信息

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

机构信息

College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.

出版信息

Bioorg Med Chem. 2009 May 15;17(10):3557-67. doi: 10.1016/j.bmc.2009.04.010. Epub 2009 Apr 11.

DOI:10.1016/j.bmc.2009.04.010
PMID:19398205
Abstract

We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent (45)Ca(2+) uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC(50) of 57 nM. The synthesis and structure-activity relationship of the diarylalkyl amides are also described.

摘要

我们已经开发出一类新型的二芳基烷基酰胺作为新型TRPV1拮抗剂。它们在大鼠背根神经节神经元中表现出强大的（45）Ca（2+）摄取抑制作用。特别是，酰胺59被鉴定为一种强效拮抗剂，IC（50）为57 nM。本文还描述了二芳基烷基酰胺的合成及其构效关系。

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