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肟碳酸酯——新型 FAAH 抑制剂的发现。

Oxime carbamate--discovery of a series of novel FAAH inhibitors.

机构信息

Department of Chemistry, Bristol-Myers Squibb Research & Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.

出版信息

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1272-7. doi: 10.1016/j.bmcl.2009.11.080. Epub 2009 Nov 24.

Abstract

A series of novel oxime carbamates have been identified as potent inhibitors of the key regulatory enzyme of the endocannabinoid signaling system, fatty acid amide hydrolase (FAAH). In this Letter, the rationale behind the discovery and the biological evaluations of this novel class of FAAH inhibitors are presented. Both in vitro and in vivo results of selected targets are discussed, along with inhibition kinetics and molecular modeling studies.(1).

摘要

一系列新型肟基氨基甲酸酯已被鉴定为内源性大麻素信号系统关键调节酶——脂肪酸酰胺水解酶(FAAH)的有效抑制剂。在本信中,介绍了发现这种新型 FAAH 抑制剂的基本原理和生物学评估。讨论了选定靶标的体外和体内结果,以及抑制动力学和分子建模研究。

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