- N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
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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.
- Sunduru, Naresh,Svensson, Mona,Cipriano, Mariateresa,Marwaha, Sania,Andersson, C. David,Svensson, Richard,Fowler, Christopher J.,Elofsson, Mikael
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p. 513 - 521
(2017/11/10)
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- 3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis
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A whole organism high-throughput screen of approximately 87,000 compounds against Trypanosoma brucei brucei led to the recent discovery of several novel compound classes with low micromolar activity against this organism and without appreciable cytotoxici
- Ferrins, Lori,Rahmani, Rapha?l,Sykes, Melissa L.,Jones, Amy J.,Avery, Vicky M.,Teston, Eliott,Almohaywi, Basmah,Yin, JieXiang,Smith, Jason,Hyland, Chris,White, Karen L.,Ryan, Eileen,Campbell, Michael,Charman, Susan A.,Kaiser, Marcel,Baell, Jonathan B.
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p. 450 - 465
(2013/10/01)
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- Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators
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SIRT1 is an NAD+-dependent protein deacetylase that appears to produce beneficial effects on metabolic parameters such as glucose and insulin homeostasis. Activation of SIRT1 by resveratrol (1) has been shown to modulate insulin resistance, increase mitochondrial content and prolong survival in lower organisms and in mice on a high fat diet. Herein, we describe the identification and SAR of a series of oxazolo[4,5-b]pyridines as novel small molecule activators of SIRT1 which are structurally unrelated to and more potent than resveratrol.
- Bemis, Jean E.,Vu, Chi B.,Xie, Roger,Nunes, Joseph J.,Ng, Pui Yee,Disch, Jeremy S.,Milne, Jill C.,Carney, David P.,Lynch, Amy V.,Jin, Lei,Smith, Jesse J.,Lavu, Siva,Iffland, Andre,Jirousek, Michael R.,Perni, Robert B.
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scheme or table
p. 2350 - 2353
(2009/12/03)
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- N-PHENYL BENZAMIDE DERIVATIVES AS SIRTUIN MODULATORS
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Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treatin and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Page/Page column 28
(2008/06/13)
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- Anti-inflammatory oxazole[4,5-b]pyridines
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The various isomers of oxazolo- and thiazolopyridines having utility as antiinflammatory, antipyretic and analgesic agents are prepared by condensation of an appropriate amino-hydroxypyridine or amino-mercaptopyridine with a carboxylic acid, halide or anhydride.
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