烯醇氨基甲酸酯作为脂肪酸酰胺水解酶（FAAH）的抑制剂，对FAAH具有比对内源性大麻素系统的其他靶点更高的选择性。 - Suppr

Enol carbamates as inhibitors of fatty acid amide hydrolase (FAAH) endowed with high selectivity for FAAH over the other targets of the endocannabinoid system.

作者信息

Gattinoni Sonia, De Simone Chiara, Dallavalle Sabrina, Fezza Filomena, Nannei Raffaella, Amadio Daniele, Minetti Patrizia, Quattrociocchi Gianandrea, Caprioli Antonio, Borsini Franco, Cabri Walter, Penco Sergio, Merlini Lucio, Maccarrone Mauro

机构信息

DISMA, Università degli Studi di Milano, Via Celoria 2, 20133 Milano, Italy.

出版信息

ChemMedChem. 2010 Mar 1;5(3):357-60. doi: 10.1002/cmdc.200900472.

DOI:10.1002/cmdc.200900472

PMID:20112328

Abstract

摘要

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Enol carbamates as inhibitors of fatty acid amide hydrolase (FAAH) endowed with high selectivity for FAAH over the other targets of the endocannabinoid system.烯醇氨基甲酸酯作为脂肪酸酰胺水解酶（FAAH）的抑制剂，对FAAH具有比对内源性大麻素系统的其他靶点更高的选择性。

ChemMedChem. 2010 Mar 1;5(3):357-60. doi: 10.1002/cmdc.200900472.

A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.一类新型肟基氨基甲酸酯类化合物作为脂肪酸酰胺水解酶的可逆抑制剂。

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4406-11. doi: 10.1016/j.bmcl.2010.06.050. Epub 2010 Jun 15.

Oxime carbamate--discovery of a series of novel FAAH inhibitors.肟碳酸酯——新型 FAAH 抑制剂的发现。

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

Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.从生物活性分子中挖掘脂肪酸酰胺水解酶（FAAH）抑制剂：苯丁锡和安比西林被鉴定为 FAAH 抑制剂。

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6793-6. doi: 10.1016/j.bmcl.2009.09.086. Epub 2009 Sep 30.

Design, synthesis, and in vitro evaluation of carbamate derivatives of 2-benzoxazolyl- and 2-benzothiazolyl-(3-hydroxyphenyl)-methanones as novel fatty acid amide hydrolase inhibitors.2-苯并恶唑基-和2-苯并噻唑基-(3-羟基苯基)-甲酮氨基甲酸酯衍生物作为新型脂肪酸酰胺水解酶抑制剂的设计、合成及体外评价

J Med Chem. 2007 Aug 23;50(17):4236-42. doi: 10.1021/jm070501w. Epub 2007 Aug 1.

3-Heterocycle-phenyl N-alkylcarbamates as FAAH inhibitors: design, synthesis and 3D-QSAR studies.3-杂环苯基 N-烷基氨基甲酸酯作为 FAAH 抑制剂的设计、合成及 3D-QSAR 研究。

ChemMedChem. 2010 Feb 1;5(2):213-31. doi: 10.1002/cmdc.200900390.

Chiral 3-(4,5-dihydrooxazol-2-yl)phenyl alkylcarbamates as novel FAAH inhibitors: Insight into FAAH enantioselectivity by molecular docking and interaction fields.手性3-(4,5-二氢恶唑-2-基)苯基烷基氨基甲酸酯作为新型脂肪酸酰胺水解酶抑制剂：通过分子对接和相互作用场深入了解脂肪酸酰胺水解酶的对映选择性

Eur J Med Chem. 2009 Oct;44(10):4179-91. doi: 10.1016/j.ejmech.2009.05.012. Epub 2009 May 22.

Understanding the role of carbamate reactivity in fatty acid amide hydrolase inhibition by QM/MM mechanistic modelling.运用 QM/MM 机理模型理解氨基甲酸酯反应性在脂肪酸酰胺水解酶抑制中的作用。

Chem Commun (Camb). 2011 Mar 7;47(9):2517-9. doi: 10.1039/c0cc04937a. Epub 2011 Jan 14.

Design of on-target FAAH inhibitors.靶向脂肪酸酰胺水解酶（FAAH）抑制剂的设计。

Chem Biol. 2005 Nov;12(11):1157-8. doi: 10.1016/j.chembiol.2005.11.001.

Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.作为脂肪酸酰胺水解酶抑制剂的3'-或4'-取代联苯-3-基酯环己基甲酸：合成、定量构效关系及分子模拟研究

J Med Chem. 2004 Oct 7;47(21):4998-5008. doi: 10.1021/jm031140x.

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In Silico and In Vitro Analysis of Major Cannabis-Derived Compounds as Fatty Acid Amide Hydrolase Inhibitors.计算机模拟和体外分析大麻衍生化合物作为脂肪酸酰胺水解酶抑制剂。

Molecules. 2020 Dec 24;26(1):48. doi: 10.3390/molecules26010048.

The endocannabinoid hydrolase FAAH is an allosteric enzyme.内源性大麻素水解酶 FAAH 是一种变构酶。

Sci Rep. 2020 Feb 10;10(1):2292. doi: 10.1038/s41598-020-59120-1.

Role of Steroids on the Membrane Binding Ability of Fatty Acid Amide Hydrolase.类固醇对脂肪酸酰胺水解酶膜结合能力的作用。

Cannabis Cannabinoid Res. 2019 Mar 13;4(1):42-50. doi: 10.1089/can.2018.0051. eCollection 2019.

The selective reversible FAAH inhibitor, SSR411298, restores the development of maladaptive behaviors to acute and chronic stress in rodents.选择性可逆 FAAH 抑制剂 SSR411298 可恢复啮齿动物对急性和慢性应激的适应不良行为的发展。

Sci Rep. 2018 Feb 5;8(1):2416. doi: 10.1038/s41598-018-20895-z.

Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474.基于活性的蛋白质谱分析揭示了脂肪酸酰胺水解酶抑制剂BIA 10-2474的脱靶蛋白。

Science. 2017 Jun 9;356(6342):1084-1087. doi: 10.1126/science.aaf7497.

Cannabinoid CB receptor ligand profiling reveals biased signalling and off-target activity.大麻素 CB 受体配体分析揭示了偏向信号和脱靶活性。

Nat Commun. 2017 Jan 3;8:13958. doi: 10.1038/ncomms13958.

Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase: New Targets for Future Antidepressants.脂肪酸酰胺水解酶和单酰甘油脂肪酶抑制剂：未来抗抑郁药的新靶点。

Curr Neuropharmacol. 2015;13(6):760-75. doi: 10.2174/1570159x13666150612225212.

The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity.新型口服可用且外周受限的选择性大麻素CB2受体激动剂LEI-101可预防顺铂诱导的肾毒性。

Br J Pharmacol. 2016 Feb;173(3):446-58. doi: 10.1111/bph.13338. Epub 2016 Jan 15.

Potential Therapeutic Value of a Novel FAAH Inhibitor for the Treatment of Anxiety.一种新型脂肪酸酰胺水解酶（FAAH）抑制剂治疗焦虑症的潜在治疗价值。

PLoS One. 2015 Sep 11;10(9):e0137034. doi: 10.1371/journal.pone.0137034. eCollection 2015.

Chemical probes of endocannabinoid metabolism.内源性大麻素代谢的化学探针。

Pharmacol Rev. 2013 Mar 19;65(2):849-71. doi: 10.1124/pr.112.006387. Print 2013 Apr.

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Enol carbamates as inhibitors of fatty acid amide hydrolase (FAAH) endowed with high selectivity for FAAH over the other targets of the endocannabinoid system.

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