116489-65-7Relevant 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)
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.
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
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.
, p. 450 - 465 (2013/10/01)
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