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 IC50 of 2.6 µM as a chemical starting point for...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2017-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/14756366.2016.1265520 |
| _version_ | 1818216451089104896 |
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| author | Naresh Sunduru Mona Svensson Mariateresa Cipriano Sania Marwaha C. David Andersson Richard Svensson Christopher J. Fowler Mikael Elofsson |
| author_facet | Naresh Sunduru Mona Svensson Mariateresa Cipriano Sania Marwaha C. David Andersson Richard Svensson Christopher J. Fowler Mikael Elofsson |
| author_sort | Naresh Sunduru |
| collection | DOAJ |
| 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 IC50 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 IC50 of 0.35 µM. |
| first_indexed | 2024-12-12T06:52:11Z |
| format | Article |
| id | doaj.art-56045177574f429a8dafbbdc15fb8d71 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-12-12T06:52:11Z |
| publishDate | 2017-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-56045177574f429a8dafbbdc15fb8d712022-12-22T00:34:03ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742017-01-0132151352110.1080/14756366.2016.12655201265520N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitorsNaresh Sunduru0Mona Svensson1Mariateresa Cipriano2Sania Marwaha3C. David Andersson4Richard Svensson5Christopher J. Fowler6Mikael Elofsson7Umeå UniversityUmeå UniversityUmeå UniversityUmeå UniversityUmeå UniversityUppsala UniversityUmeå UniversityUmeå UniversityFatty 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 IC50 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 IC50 of 0.35 µM.http://dx.doi.org/10.1080/14756366.2016.1265520Fatty acid amide hydrolase inhibitorsendocannabinoid systemoxazolo[4,5-b]pyridine anilines1H-imidazo[4,5-b]pyridine anilines |
| spellingShingle | Naresh Sunduru Mona Svensson Mariateresa Cipriano Sania Marwaha C. David Andersson Richard Svensson Christopher J. Fowler Mikael Elofsson N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors Journal of Enzyme Inhibition and Medicinal Chemistry Fatty acid amide hydrolase inhibitors endocannabinoid system oxazolo[4,5-b]pyridine anilines 1H-imidazo[4,5-b]pyridine anilines |
| 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 | Fatty acid amide hydrolase inhibitors endocannabinoid system oxazolo[4,5-b]pyridine anilines 1H-imidazo[4,5-b]pyridine anilines |
| url | http://dx.doi.org/10.1080/14756366.2016.1265520 |
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