844498-87-9Relevant articles and documents
The discovery of a selective, high affinity A2B adenosine receptor antagonist for the potential treatment of asthma
Zablocki, Jeff,Kalla, Rao,Perry, Thao,Palle, Venkata,Varkhedkar, Vaibhav,Xiao, Dengming,Piscopio, Anthony,Maa, Tenning,Gimbel, Art,Hao, Jia,Chu, Nancy,Leung, Kwan,Zeng, Dewan
, p. 609 - 612 (2007/10/03)
Adenosine has been suggested to play a role in asthma, possibly via activation of A2B adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A2B AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A2B AdoR antagonist with good selectivity (A2B AdoR Ki = 50 nM, selectivity A1 > 200: A2A > 200: A3 > 167).
CVT-4325: A potent fatty acid oxidation inhibitor with favorable oral bioavailability
Elzein, Elfatih,Ibrahim, Prabha,Koltun, Dmitry O.,Rehder, Ken,Shenk, Kevin D.,Marquart, Timothy A.,Jiang, Bob,Li, Xiaofen,Natero, Reina,Li, Yuan,Nguyen, Marie,Kerwar, Suresh,Chu, Nancy,Soohoo, Daniel,Hao, Jia,Maydanik, Victoria Y.,Lustig, David A.,Zeng, Dewan,Leung, Kwan,Zablocki, Jeff A.
, p. 6017 - 6021 (2007/10/03)
New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325, a potent FOXi (IC50 = 380 nM, rat mitochondria) with favorable PK properties (F = 93%, t1/2 = 13.6 h, dog). New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50 = 380 nM rat mitochondria) with favorable PK properties (F = 93%, t1/2 = 13.6 h, dog).
