Discovery of potent, non-carbonyl inhibitors of fatty acid amide hydrolase (FAAH)

被引：6

作者：

Gowlugari, Sumithra ^{[1
]}

DeFalco, Jeff ^{[1
]}

Nguyen, Margaret T. ^{[1
]}

Kaub, Carl ^{[1
]}

Chi, Candace ^{[1
]}

Duncton, Matthew A. J. ^{[1
]}

Emerling, Daniel E. ^{[1
]}

Kelly, Michael G. ^{[1
]}

Kincaid, John ^{[1
]}

Vincent, Fabien ^{[1
]}

机构：

[1] Renovis Inc, San Francisco, CA 94080 USA

来源：

MEDCHEMCOMM | 2012年 / 3卷 / 10期

关键词：

SELECTIVITY; ANANDAMIDE; MECHANISMS; ANALGESIA; SYSTEM;

D O I：

10.1039/c2md20146a

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) inhibition is a promising target for the treatment of pain, anxiety and depression. The vast majority of FAAH inhibitors contain an electrophilic moiety and are known to react covalently with the enzyme. Herein we present the discovery of potent inhibitors, such as RN-450 29, which are based upon a novel tetrahydropyridopyridine scaffold lacking an obvious electrophilic site, and which appear to inhibit FAAH in a reversible and non-covalent manner.

引用

页码：1258 / 1263

页数：6

共 50 条

[21] Effects of fatty acid amide hydrolase (FAAH) inhibitors on working memory in rats
Leigh V. Panlilio
Eric B. Thorndike
Spyros P. Nikas
Shakiru O. Alapafuja
Tiziano Bandiera
Benjamin F. Cravatt
Alexandros Makriyannis
Daniele Piomelli
Steven R. Goldberg
Zuzana Justinova
Psychopharmacology, 2016, 233 : 1879 - 1888
[22] Dual soluble Epoxide Hydrolase (sEH) and Fatty Acid Amide Hydrolase (FAAH) inhibitors for treating
Kodani, Sean
Wagner, Karen
Hwang, Sung Hee
Lee, Kin
Morisseau, Christophe
Hammock, Bruce
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2017, 253
[23] Modulation of angiogenesis by the fatty acid amide hydrolase (FAAH)
Koester, S.
Rieck, S.
Vosen, S.
Matthey, M.
Meyer, J.
Schmitz-Valckenberg, S.
Fleischmann, B.
Wenzel, D.
ACTA PHYSIOLOGICA, 2014, 210 : 120 - 120
[24] Inhibition of Fatty Acid Amide Hydrolase (FAAH) by Macamides
M. Alasmari
M. Bӧhlke
C. Kelley
T. Maher
A. Pino-Figueroa
Molecular Neurobiology, 2019, 56 : 1770 - 1781
[25] Inhibition of Fatty Acid Amide Hydrolase (FAAH) by Macamides
Alasmari, M.
Bohlke, M.
Kelley, C.
Maher, T.
Pino-Figueroa, A.
MOLECULAR NEUROBIOLOGY, 2019, 56 (03) : 1770 - 1781
[26] Inhibition of Fatty Acid Amide Hydrolase (FAAH) by Macamides
Alasmari, Moudi M.
Bohlke, M.
Kelley, C.
Maher, T.
Pino-Figueroa, A.
FASEB JOURNAL, 2018, 32 (01):
[27] Latest advances in the discovery of fatty acid amide hydrolase inhibitors
Bisogno, Tiziana
Maccarrone, Mauro
EXPERT OPINION ON DRUG DISCOVERY, 2013, 8 (05) : 509 - 522
[28] Design, synthesis, and in vitro evaluation of novel inhibitors of fatty acid amide hydrolase (FAAH)
Cramer, Sarah
Johnson, Jacklyn
El-Alfy, Abir
Stec, Jozef
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2015, 249
[29] Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain
Meyers, Marvin J.
Long, Scott A.
Pelc, Matthew J.
Wang, Jane L.
Bowen, Scott J.
Schweitzer, Barbara A.
Wilcox, Mark V.
McDonald, Joseph
Smith, Sarah E.
Foltin, Susan
Rumsey, Jeanne
Yang, Young-Sun
Walker, Mark C.
Kamtekar, Satwik
Beidler, David
Thorarensen, Atli
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (21) : 6545 - 6553
[30] Effect of Fatty Acid Amide Hydrolase (FAAH) Inhibitors Isolated from Nutmeg on Anxiety
El-Alfy, Abir T.
Jeon, Andrew
An, Hea Re
Kendrek, Jennifer
Abourashed, Ehab
FASEB JOURNAL, 2017, 31

← 1 2 3 4 5 →