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

نویسندگان

  • Naresh Sunduru
  • Mona Svensson
  • Mariateresa Cipriano
  • Sania Marwaha
  • C David Andersson
  • Richard Svensson
  • Christopher J Fowler
  • Mikael Elofsson
چکیده

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.

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عنوان ژورنال:
  • Journal of enzyme inhibition and medicinal chemistry

دوره 32 1  شماره 

صفحات  -

تاریخ انتشار 2017