52333-90-1Relevant articles and documents
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
, p. 513 - 521 (2017/11/10)
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.
Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators
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.
scheme or table, p. 2350 - 2353 (2009/12/03)
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.
Anti-inflammatory oxazole[4,5-b]pyridines
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, (2008/06/13)
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.