951-73-5Relevant academic research and scientific papers
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.
An alternate approach for the synthesis of 2-substituted-arylimidazo[4,5-b] pyridines and their anti-bacterial activity
Vinodkumar, Ramanatham,Chari, Murugulla Adharvana,Dubey, Pramod Kumar
, p. 1537 - 1541 (2008/09/18)
(Chemical Equation Presented) An alternate method for the convenient preparation of the imidazo[4,5-b]pyridines from 2,3-pyridinediamine and 2-aryl-3(1)-benzoxazine-4H-onehas been illustrated. The mechanistic pathway for the formation of the product 4 has been proposed. All the compounds prepared herein were screened for their anti- bacterial properties.
Reaction of isatoic anhydride with bifunctional reagents: Synthesis of some new quinazolone fused heterocycles, 2-substituted anilinoheterocyclic derivatives and other related compounds
Fadda,Refat,Zaki,Monir
, p. 3537 - 3545 (2007/10/03)
A new synthesis of quinazolone fused heterocycles (2, 5, 8), anilinoheterocycles (4, 7, 10, 12, 14) and substituted 2-aminoquinoline (15, 16) based on the reaction of isatoic anhydride (1) with different active bifunctional compounds in presence of glacial acetic acid and freshly fused sodium acetate is described. Structures of the newly prepared compounds are established by chemical and spectral data.
Studies on the condensation of 2, 3-pyridinediamines with 2-phenyl-3, 1- benzoxazin-4(H)-one
Dubey,Kumar, R. Vinod
, p. 732 - 734 (2007/10/03)
The reaction of 2, 3-pyridinediamine 1a and its 5-bromo analogue 1b with 2-phenyl-3,l-benzoxazin-4(H)-one 2 in refluxing acetic acid leads to the formation of 2-(2'-N-benzoyl-aminophenyl)imidazo[4, 5-b]pyridine 3a and 6- bromo-2-(2'-N-benzoylaminophenyl)i
Cyclic Nucleotide Phosphodiesterase Inhibition by Imidazopyridines: Analogues of Sulmazole and Isomazole as Inhibitors of the cGMP Specific Phosphodiesterase
Coates, William J.,Connolly, Brendan,Dhanak, Dashyant,Flynn, Sean T.,Worby, Angela
, p. 1387 - 1392 (2007/10/02)
The synthesis and phosphodiesterase (PDE) inhibitory profile of a series of imidazopyridines, including sulmazole and isomazole, on separated PDE isoenzymes are described.The results show that both sulmazole and isomazole are weak inhibitors of PDE III, and their inotropic activity is unlikely to be due to PDE III inhibition alone.Surprisingly, both compounds were found to be significant inhibitors of the cGMP specific isoenzyme, PDE V, and a series of simple 2-substituted phenylimidazopyridines have been made to investigate the SAR of PDE activity.This has been shown to be sensitive to chain length, polarity, and the nature of the heteroatom linking group.Potent PDE V inhibitors, many of which are also significant inhibitors of PDE IV, have been identified.
