[EN] DISUBSTITUTED BETA-LACTONES AS INHIBITORS OF N-ACYLETHANOLAMINE ACID AMIDASE (NAAA)<br/>[FR] BÊTA-LACTONES DISUBSTITUÉS EN TANT QU'INHIBITEURS DE L'AMIDASE ACIDE DE N-ACYLÉTHANOLAMINE (NAAA)
申请人:UNIV CALIFORNIA
公开号:WO2013078430A1
公开(公告)日:2013-05-30
The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.
Structural confirmation of the dihydrosphinganine and fatty acid constituents of the dental pathogen Porphyromonas gingivalis
作者:JiYoung Mun、Amber Onorato、Frank C. Nichols、Martha D. Morton、Abdullah I. Saleh、Morgan Welzel、Michael B. Smith
DOI:10.1039/b712707c
日期:——
Porphyromonas gingivalis, a recognized periodontal pathogen, is a source of sphinganine bases, fatty acids, free ceramides as well as complex lipids that potentiate interleukin-1b-mediated secretory responses in gingival fibroblasts. The purpose of this study is the structural verification of the sphinganine bases and fatty acids that had been proposed as major components of the complex lipids found in P. gingivalis. The putative C17, C18, and C19 sphinganine bases were prepared from Garner's aldehyde (1) or from a protected serine Weinreb's amide (2). We confirmed that isobranched sphinganine bases are the major structural feature of the ceramides observed from P. gingivalis. We also prepared a C17 unsaturated fatty acid, along with an isobranched C17 3-hydroxy fatty acid, and determined that the major component of the active lipids was the latter.
SYNTHESIS OF FLUOROARACHIDONIC ACID AND METHODS OF USE THEREOF
申请人:The United States of America, as represented by the Secretary, Department of Health and Human Serv
公开号:US20130302247A1
公开(公告)日:2013-11-14
There are provided, inter alia, methods for diagnosis of the extent of neuroinflammation in a subject. The methods include administering an
18
F-labeled arachidonic acid to a subject in need thereof, obtaining a positron emission tomography (PET) scan of the subject, and determine the extent of neuroinflammation from the PET scan. There are provided, inter alia, methods of synthesis of reagents useful for the production of an
18
F-labeled arachidonic acid.
申请人:Iowa State University Research Foundation, Inc.
公开号:US20130303795A1
公开(公告)日:2013-11-14
The present invention relates to methods for making a fatty acid N-acylalkanolamine having the formula:
One of the methods comprises the steps of providing a vinyl ester of a fatty acid having the formula:
providing a primary or secondary alkanolamine having the formula: NHR
1
R
2
; and reacting the vinyl ester of the fatty acid with the alkanolamine under conditions effective to form the fatty acid N-acylalkanolamine. The other method comprises the steps of providing a fatty acid; purifying the fatty acid; providing a primary or secondary alkanolamine having the formula: NHR
1
R
2
; reacting the fatty acid with the alkanolamine under conditions effective to form the fatty acid N-acylalkanolamine; and purifying the formed fatty acid N-acylalkanolamine.
Substituted Heterocyclic Derivative, Preparation Method And Use Thereof
申请人:Xiamen University
公开号:US20170334896A1
公开(公告)日:2017-11-23
The invention provides a compound as shown by Formula I having an enzyme activity which can inhibit endocannabinoid hydrolases NAAA and/or FAAH, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and a preparation method and a use of the compound.