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

被引：13

作者：

Li, Fu-Nan ^{[1
]}

Kim, Nam-Jung ^{[1
]}

Paek, Seung-Mann ^{[1
]}

Kwon, Do-Yeon ^{[1
]}

Min, Kyung Hoon ^{[2
]}

Jeong, Yeon-Su ^{[3
]}

Kim, Sun-Young ^{[3
]}

Park, Young-Ho ^{[3
]}

Kim, Hee-Doo ^{[4
]}

Park, Hyeung-Geun ^{[1
]}

Suh, Young-Ger ^{[1
]}

机构：

[1] Seoul Natl Univ, Coll Pharm, Seoul 151742, South Korea

[2] Chung Ang Univ, Coll Pharm, Seoul 156756, South Korea

[3] Amorepacific R&D Ctr, Yongin 446729, Gyeonggi Do, South Korea

[4] Sookmyung Womens Univ, Coll Pharm, Seoul 140742, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 10期

关键词：

Diarylalkyl amides; TRPV1; antagonists; VANILLOID RECEPTOR-1; NEUROPATHIC PAIN; CAPSAICIN CREAM; POTENT; EXPRESSION; CONVERSION; DISCOVERY; THIOUREAS; NEURONS; CHANNEL;

D O I：

10.1016/j.bmc.2009.04.010

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：3557 / 3567

页数：11

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