N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors

Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat neurological diseases. In search of new FAAH inhibitors, we identified 2-(4-cyclohexylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4g, with an IC(50) of 2.6 µM as a chemical starting point fo...

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Autores principales: Sunduru, Naresh, Svensson, Mona, Cipriano, Mariateresa, Marwaha, Sania, Andersson, C. David, Svensson, Richard, Fowler, Christopher J., Elofsson, Mikael
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009913/
https://www.ncbi.nlm.nih.gov/pubmed/28114819
http://dx.doi.org/10.1080/14756366.2016.1265520
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author Sunduru, Naresh
Svensson, Mona
Cipriano, Mariateresa
Marwaha, Sania
Andersson, C. David
Svensson, Richard
Fowler, Christopher J.
Elofsson, Mikael
author_facet Sunduru, Naresh
Svensson, Mona
Cipriano, Mariateresa
Marwaha, Sania
Andersson, C. David
Svensson, Richard
Fowler, Christopher J.
Elofsson, Mikael
author_sort Sunduru, Naresh
collection PubMed
description Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat neurological diseases. In search of new FAAH inhibitors, we identified 2-(4-cyclohexylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4g, with an IC(50) of 2.6 µM as a chemical starting point for the development of potent FAAH inhibitors. Preliminary hit-to-lead optimisation resulted in 2-(4-phenylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4i, with an IC(50) of 0.35 µM.
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spelling pubmed-60099132018-07-11 N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors Sunduru, Naresh Svensson, Mona Cipriano, Mariateresa Marwaha, Sania Andersson, C. David Svensson, Richard Fowler, Christopher J. Elofsson, Mikael J Enzyme Inhib Med Chem Short Communication Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat neurological diseases. In search of new FAAH inhibitors, we identified 2-(4-cyclohexylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4g, with an IC(50) of 2.6 µM as a chemical starting point for the development of potent FAAH inhibitors. Preliminary hit-to-lead optimisation resulted in 2-(4-phenylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4i, with an IC(50) of 0.35 µM. Taylor & Francis 2017-01-23 /pmc/articles/PMC6009913/ /pubmed/28114819 http://dx.doi.org/10.1080/14756366.2016.1265520 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/Licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/Licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Short Communication
Sunduru, Naresh
Svensson, Mona
Cipriano, Mariateresa
Marwaha, Sania
Andersson, C. David
Svensson, Richard
Fowler, Christopher J.
Elofsson, Mikael
N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
title N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
title_full N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
title_fullStr N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
title_full_unstemmed N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
title_short N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
title_sort n-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (faah) inhibitors
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009913/
https://www.ncbi.nlm.nih.gov/pubmed/28114819
http://dx.doi.org/10.1080/14756366.2016.1265520
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