ω-Heteroarylalkylcarbamates as inhibitors of fatty acid amide hydrolase (FAAH)

被引：4
|
作者：
Terwege, Tobias [1 ]
Dahlhaus, Helmut [1 ]
Hanekamp, Walburga [1 ]
Lehr, Matthias [1 ]
机构：
[1] Univ Munster, Inst Pharmaceut & Med Chem, D-48149 Munster, Germany
来源：
MEDCHEMCOMM | 2014年 / 5卷 / 07期
关键词：
CANNABINOID RECEPTORS; DUAL INHIBITORS; SYSTEM; ENDOCANNABINOIDS; DEGRADATION; ANANDAMIDE; HYDROLYSIS; STABILITY;
D O I：
10.1039/c4md00181h
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：
Fatty acid amide hydrolase (FAAH) is a serine hydrolase that terminates the analgetic and anti-inflammatory effects of endocannabinoids such as anandamide. Herein we describe structure-activity relationship studies on a new series of omega-heteroarylalkylcarbamate inhibitors of FAAH. The most active compounds exhibit IC50 values in the low nanomolar range. Investigations on selectivity and metabolic stability of these inhibitors are also presented.
引用
收藏
页码：932 / 936
页数：5
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