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杂环连接的苯苄基酰胺类新型 TRPV1 拮抗剂及其 TRPV1 结合模式：约束诱导增强体外和体内活性。

Heterocycle-linked phenylbenzyl amides as novel TRPV1 antagonists and their TRPV1 binding modes: constraint-induced enhancement of in vitro and in vivo activities.

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

Chem Asian J. 2013 Feb;8(2):400-9. doi: 10.1002/asia.201200730. Epub 2012 Dec 3.

DOI:10.1002/asia.201200730
PMID:23208797
Abstract

A series of heterocycle-linked constrained phenylbenzyl amides were found to be TRPV1 antagonists with promising in vivo profiles. In particular, one of the analogues containing a furan linker exhibited excellent TRPV1 antagonistic activity and in vivo analgesic efficacy. In addition, the binding modes of dibenzyl thiourea, benzylphenethyl amide, and furan-linked phenylbenzyl amide were examined by using the flexible docking study within the rTRPV1 homology model.

摘要

研究发现，一系列杂环连接的受限苯并苄基酰胺是 TRPV1 拮抗剂，具有良好的体内特性。特别是，含有呋喃连接基的类似物表现出优异的 TRPV1 拮抗活性和体内镇痛功效。此外，还通过在 rTRPV1 同源模型内进行柔性对接研究，考察了二苄基硫脲、苄基苯乙酰胺和呋喃连接的苯并苄基酰胺的结合模式。

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